Innovative 𝐂𝐡𝐢𝐫𝐚𝐥 𝐌𝐞𝐭𝐚𝐥-𝐎𝐫𝐠𝐚𝐧𝐢𝐜 𝐂𝐚𝐠𝐞-Based Chiral Stationary Phases for Enhanced HPLC Enantioseparation

Metal-organic cages (MOCs) are emerging porous materials with unique properties, such as good stability and well-defined cavities. Chiral MOCs show promise in enantiomeric recognition and separation, but their use as chiral stationary phases (CSPs) for high-performance liquid chromatography (HPLC) enantioseparation remains underexplored.

𝐔𝐧𝐝𝐞𝐫𝐬𝐭𝐚𝐧𝐝𝐢𝐧𝐠 𝐂𝐡𝐢𝐫𝐚𝐥 𝐁𝐢𝐨𝐞𝐪𝐮𝐢𝐯𝐚𝐥𝐞𝐧𝐜𝐞: A Must for Modern Drug Development

Did you know that many drugs exist as mirror-image molecules, or enantiomers, that can have drastically different effects in the body? Chiral bioequivalence studies are critical to ensuring that patients receive safe and effective medications, especially when only one enantiomer (eutomer) provides therapeutic benefits while the other (distomer) may be inactive - or even harmful.

𝐂𝐡𝐢𝐫𝐚𝐥 𝐥𝐢𝐪𝐮𝐢𝐝 𝐜𝐫𝐲𝐬𝐭𝐚𝐥𝐬: 𝐓𝐨𝐰𝐚𝐫𝐝𝐬 𝐆𝐫𝐞𝐞𝐧𝐞𝐫 𝐞𝐧𝐚𝐧𝐭𝐢𝐨𝐬𝐞𝐥𝐞𝐜𝐭𝐢𝐯𝐞 𝐋𝐂 - An exploratory study

# Replacement of acetonitrile with alternative solvents in enantioselective chromatography.
# First use of propylene carbonate and methylal in enantioselective chromatography.
# Separation of liquid crystals on immobilized amylose tris(3-chloro-5- methylcarbamate).
# Impact of flow rate on column efficiency with green solvents compared to acetonitrile.

𝐎𝐧 𝐭𝐡𝐞 (𝐈𝐦)𝐩𝐨𝐬𝐬𝐢𝐛𝐥𝐞 𝐈𝐧𝐭𝐞𝐫𝐩𝐥𝐚𝐲𝐬 𝐁𝐞𝐭𝐰𝐞𝐞𝐧 𝐍𝐚𝐭𝐮𝐫𝐚𝐥 𝐚𝐧𝐝 𝐌𝐚𝐠𝐧𝐞𝐭𝐢𝐜 𝐎𝐩𝐭𝐢𝐜𝐚𝐥 𝐀𝐜𝐭𝐢𝐯𝐢𝐭𝐲 𝐢𝐧 𝐂𝐡𝐢𝐫𝐚𝐥 𝐒𝐚𝐦𝐩𝐥𝐞𝐬

Observing both natural and magnetic optical activity in chiral samples is fascinating. However, if we’re not careful, it can lead to misinterpreting the data. Starting from basic, broad principles, we’ll explain what effects you might see and which ones you won’t in these situations.

𝐖𝐡𝐞𝐭𝐡𝐞𝐫 𝐖𝐞 𝐀𝐫𝐞 𝐀𝐥𝐨𝐧𝐞: Can Chirality Answer

Detecting biosignatures of extraterrestrial life is a primary scientific objective. Current detection methods focus on key molecular classes fundamental to terrestrial biology. A more universally applicable approach could involve searching for homochiral molecules, which are critical in the origin of life.

𝐋𝐚𝐜𝐭𝐚𝐦 𝐒𝐜𝐚𝐟𝐟𝐨𝐥𝐝 𝐓𝐨𝐰𝐚𝐫𝐝𝐬 𝐕𝐚𝐫𝐢𝐞𝐝 𝐌𝐞𝐝𝐢𝐜𝐢𝐧𝐚𝐥 𝐀𝐩𝐩𝐥𝐢𝐜𝐚𝐭𝐢𝐨𝐧𝐬

A Must-Read for Medicinal and Chiral Chemists: Dive into the Fascinating World of β-Lactam Scaffolds

𝐂𝐨𝐧𝐬𝐭𝐫𝐮𝐜𝐭𝐢𝐨𝐧 𝐨𝐟 𝐂𝐡𝐢𝐫𝐚𝐥 𝐀𝐳𝐢𝐫𝐢𝐝𝐢𝐧𝐞𝐬: Synthetic Approaches

Optically active aziridines are crucial three-membered nitrogen-heterocyclic compounds found in natural products, pharmaceuticals, and agrochemicals, serving as therapeutic frameworks and versatile synthetic endpoints. Recent breakthroughs have streamlined their synthesis, showing great potential in drug discovery. Key strategies for assembling chiral aziridines include reactions with olefins, imines, azirines, and intramolecular cyclization of amine derivatives. This review summarizes these synthetic strategies and their applications in the pharmaceutical and agrochemical industries.

𝐍𝐨𝐯𝐞𝐥 𝐂𝐡𝐢𝐫𝐚𝐥 𝐌𝐚𝐜𝐫𝐨𝐜𝐲𝐜𝐥𝐢𝐜 𝐀𝐫𝐞𝐧𝐞𝐬: Recent advances

Chiral macrocyclic arenes, with their unique three-dimensional asymmetric cavities, electron-rich structures, and luminescence properties, are significant in macrocyclic and supramolecular chemistry.

𝐀𝐝𝐯𝐚𝐧𝐜𝐞𝐬 𝐢𝐧 𝐂𝐚𝐭𝐚𝐥𝐲𝐭𝐢𝐜 𝐄𝐧𝐚𝐧𝐭𝐢𝐨𝐬𝐞𝐥𝐞𝐜𝐭𝐢𝐯𝐞 𝐓𝐫𝐚𝐧𝐬𝐟𝐨𝐫𝐦𝐚𝐭𝐢𝐨𝐧𝐬 𝐔𝐬𝐢𝐧𝐠 𝐃𝐢𝐚𝐫𝐲𝐥𝐢𝐨𝐝𝐨𝐧𝐢𝐮𝐦 𝐑𝐞𝐚𝐠𝐞𝐧𝐭𝐬

Diaryliodonium salts are crucial for incorporating aryl functionalities into organic molecules, enabling highly selective enantioselective reactions. In asymmetric catalysis, copper salts with chiral ligands are often used with these salts. The process involves oxidative addition of metal complexes to iodonium salts, followed by nucleophilic interception and reductive elimination, yielding enantioenriched products.

𝐒𝐭𝐞𝐫𝐞𝐨𝐬𝐞𝐥𝐞𝐜𝐭𝐢𝐯𝐞 𝐒𝐞𝐩𝐚𝐫𝐚𝐭𝐢𝐨𝐧 𝐨𝐟 𝐂𝐡𝐢𝐫𝐚𝐥 𝐃𝐫𝐮𝐠𝐬

In pharmaceuticals and biopharmaceuticals, chiral liquid chromatography techniques like high-performance and ultra-performance liquid chromatography are crucial for isolating, identifying, separating, and quantifying chiral isomers (enantiomers and diastereomers) due to their different biological activities. This article offers a comprehensive overview of using liquid chromatography to separate and estimate chiral compounds. Key development strategies include selecting chromatographic conditions, optimizing sample preparation, evaluating degradation pathways, establishing system suitability criteria, and conducting method validation studies. Additionally, it discusses robust and stability-indicating methods for chiral drugs and their impurities. Method validation parameters include specificity, linearity, detection limit, quantitation limit, accuracy, precision, and solution stability.

𝐖𝐡𝐲 𝐝𝐢𝐝 𝐥𝐢𝐟𝐞 "𝐭𝐮𝐫𝐧 𝐥𝐞𝐟𝐭?: 𝐍𝐀𝐒𝐀 𝐬𝐜𝐢𝐞𝐧𝐭𝐢𝐬𝐭𝐬 𝐰𝐚𝐧𝐭 𝐭𝐨 𝐬𝐨𝐥𝐯𝐞 𝐚 𝐦𝐲𝐬𝐭𝐞𝐫𝐲

Glavin, D.P., Dworkin, J.P., Alexander, C.M.O. et al. Abundant ammonia and nitrogen-rich soluble organic matter in samples from asteroid (101955) Bennu. Nat Astron (2025).

𝐂𝐡𝐢𝐫𝐚𝐥𝐢𝐭𝐲 𝐢𝐧 𝐂𝐨𝐧𝐭𝐞𝐦𝐩𝐨𝐫𝐚𝐫𝐲 𝐃𝐫𝐮𝐠 𝐃𝐢𝐬𝐜𝐨𝐯𝐞𝐫𝐲: Significance

Over half of drugs are chiral compounds, with chirality significantly impacting their interactions, safety, and efficacy. Did you know that about 90% of these compounds are marketed as racemates, which function differently in chiral environments, showing notable variances in pharmacology, toxicology, and metabolism? Recent advancements in asymmetric synthesis have heightened interest in single enantiomers for medicinal chemistry. This review compiles FDA-approved chiral medicines from 2022 and 2023, with a focus on their synthesis and chiral induction.

𝐓𝐡𝐞 𝐅𝐮𝐭𝐮𝐫𝐞 𝐨𝐟 𝐂𝐡𝐢𝐫𝐚𝐥𝐢𝐭𝐲: 𝐈𝐧𝐧𝐨𝐯𝐚𝐭𝐢𝐨𝐧𝐬 𝐚𝐧𝐝 𝐄𝐦𝐞𝐫𝐠𝐢𝐧𝐠 𝐓𝐫𝐞𝐧𝐝𝐬

Excited to dig into the cutting-edge world of chirality again? Get ready for a thrilling trip down memory lane with this captivating series, hashtag#ChiralityOnFriday (9/10)! Originally featured on Chiralpedia, this article dives into the game-changing advancements and future possibilities in chiral technology.

𝐂𝐡𝐢𝐫𝐚𝐥𝐢𝐭𝐲 𝐢𝐧 𝐌𝐚𝐭𝐞𝐫𝐢𝐚𝐥𝐬 𝐒𝐜𝐢𝐞𝐧𝐜𝐞: 𝑫𝒆𝒔𝒊𝒈𝒏𝒊𝒏𝒈 𝒘𝒊𝒕𝒉 𝑯𝒂𝒏𝒅𝒆𝒅𝒏𝒆𝒔𝒔

We're excited to revisit this gem from Chiralpedia! Check out the seventh post in our hashtag#ChiralityOnFriday series (7/10) and explore how chirality shapes materials science. From enhancing optical devices to improving catalyst selectivity, the impact of chirality is vast. This post delves into its applications, particularly in 𝐜𝐡𝐢𝐫𝐚𝐥 𝐩𝐨𝐥𝐲𝐦𝐞𝐫𝐬 and liquid crystals, and how it affects material properties and uses. Whether you're passionate about medicinal chemistry or simply curious, this read will deepen your appreciation for the critical role chirality plays in creating advanced materials with unique properties.

𝐌𝐨𝐥𝐞𝐜𝐮𝐥𝐚𝐫 𝐌𝐚𝐠𝐢𝐜 𝐛𝐞𝐡𝐢𝐧𝐝 𝐌𝐞𝐝𝐢𝐜𝐢𝐧𝐞𝐬: 𝐂𝐡𝐢𝐫𝐚𝐥𝐢𝐭𝐲 𝐢𝐧 𝐏𝐡𝐚𝐫𝐦𝐚𝐜𝐞𝐮𝐭𝐢𝐜𝐚𝐥𝐬

We're excited to revisit our past with this blog post on "💊 𝘊𝘩𝘪𝘳𝘢𝘭𝘪𝘵𝘺 𝘪𝘯 𝘗𝘩𝘢𝘳𝘮𝘢𝘤𝘦𝘶𝘵𝘪𝘤𝘢𝘭𝘴: 𝘛𝘩𝘦 𝘐𝘮𝘱𝘢𝘤𝘵 𝘰𝘧 𝘔𝘰𝘭𝘦𝘤𝘶𝘭𝘢𝘳 𝘏𝘢𝘯𝘥𝘦𝘥𝘯𝘦𝘴𝘴 𝘰𝘯 𝘔𝘦𝘥𝘪𝘤𝘪𝘯𝘦🌟" - originally featured on Chiralpedia! Dive into the sixth article of our captivating series, hashtag#ChiralityOnFriday (6/10), and explore the fascinating role of chirality in drug action and disposition.

Chiral Chemistry in Everyday Life: Hidden Handedness Around Us

Ready for some chemical magic in your daily routine? Wonder no more! Catch the brilliance of Chiralpedia with our celebrated blog post - now re-featured for your reading pleasure!

𝐂𝐡𝐢𝐫𝐚𝐥 𝐒𝐰𝐢𝐭𝐜𝐡: 𝐀𝐧 𝐄𝐧𝐥𝐢𝐠𝐡𝐭𝐞𝐧𝐢𝐧𝐠 𝐕𝐢𝐬𝐮𝐚𝐥 𝐉𝐨𝐮𝐫𝐧𝐞𝐲 𝐢𝐧𝐭𝐨 𝐒𝐢𝐧𝐠𝐥𝐞 𝐄𝐧𝐚𝐧𝐭𝐢𝐨𝐦𝐞𝐫𝐬

Hey there! The core idea of this post, "𝐂𝐡𝐢𝐫𝐚𝐥 𝐒𝐰𝐢𝐭𝐜𝐡: 𝐔𝐧𝐥𝐨𝐜𝐤𝐢𝐧𝐠 𝐭𝐡𝐞 𝐏𝐨𝐭𝐞𝐧𝐭𝐢𝐚𝐥 𝐨𝐟 𝐒𝐢𝐧𝐠𝐥𝐞 𝐄𝐧𝐚𝐧𝐭𝐢𝐨𝐦𝐞𝐫𝐬 🌟🔍" is to introduce the concept and strategy of Chiral Switch in a way that's simple and easily digestible. To make it more engaging, it’s presented visually through concept/idea maps. This blog captures the essence of how chiral switches enhance therapeutic efficacy and reduce side effects, offering readers valuable insights into their innovative potential. In today's fast-paced world, many don't have the patience or time for lengthy texts. As the saying goes, a picture is worth a thousand words! 🌟🧬

𝑪𝒂𝒑𝒕𝒊𝒗𝒂𝒕𝒊𝒏𝒈 𝒗𝒊𝒔𝒖𝒂𝒍 𝒋𝒐𝒖𝒓𝒏𝒆𝒚 𝒐𝒇 𝑪𝒉𝒊𝒓𝒂𝒍 𝑫𝒓𝒖𝒈𝒔: 𝘈𝘯 𝘪𝘯𝘷𝘪𝘵𝘦 𝘵𝘰 𝘢𝘭𝘭 𝘮𝘦𝘥𝘪𝘤𝘪𝘯𝘢𝘭 𝘢𝘯𝘥 𝘤𝘩𝘪𝘳𝘢𝘭 𝘦𝘯𝘵𝘩𝘶𝘴𝘪𝘢𝘴𝘵𝘴!

This post "𝐂𝐡𝐢𝐫𝐚𝐥 𝐃𝐫𝐮𝐠𝐬: 𝐀 𝐓𝐰𝐢𝐬𝐭𝐞𝐝 𝐓𝐚𝐥𝐞 𝐢𝐧 𝐏𝐡𝐚𝐫𝐦𝐚𝐜𝐞𝐮𝐭𝐢𝐜𝐚𝐥𝐬," takes you on an immersive journey into the fascinating world of chiral drugs. Engage with mind maps that break down complex concepts with clarity and depth. 🧠💡 The featured image – core mind map – is thoughtfully divided into two parts, ensuring you can easily navigate the intricacies of chirality. 🌐🔍 Explore the historical roots of chirality, stereochemical nomenclature system, dive into chiral pharmacology, and uncover drug toxicity case studies. 💊

The Chemistry of Taste and Smell: How Chirality Affects Senses

Revisit the brilliance of Chiralpedia with one of our beloved blog posts! This highlight is the fourth article in our ten-part series, hashtag#ChiralityOnFriday (4/10). Journey into the captivating world of chiral compounds, uncovering how they interact with our sensory receptors to shape the flavors and fragrances we encounter daily.

Chirality in Nature: From DNA to Snail Shells

Rediscover the magic as we revisit one of Chiralpedia's classic blog posts! This cherished article is the third installment in our ten-part series (3/10), hashtag#ChiralityOnFriday. Whether you're a seasoned chiral aficionado or just curious, this read is sure to enlighten and inspire. Perfectly paired with your morning coffee! ☕

Molecular Handedness: How Chirality Shapes Molecules

We're thrilled to bring back our insightful blog post, originally created for Chiralpedia! This is the second installment in our ten-part series, hashtag#ChiralityOnFriday. Chiral enthusiasts, dive into this enlightening read—it's the perfect way to start your day! ☕✨

New FDA Drug Approvals for 2024: Synthesis and Clinical Application

In 2024, the FDA approved a remarkable array of new drugs, including 32 new chemical entities (NCEs) and 18 biological entities (NBEs). Leading the charge in innovation, small-molecule chemical drugs targeted key areas like LACTB, PBP, THR-β, Raf, PDE3/4, and HIF. Monoclonal antibodies and other groundbreaking treatments followed, addressing a wide range of diseases, particularly rare conditions and cancers. Many of these drugs received accelerated approval to meet urgent medical needs.

Introduction to Chirality: Understanding the Basics

Step back into our illuminating blog series, hashtag#ChiralityOnFriday, originally crafted for Chiralpedia! This first installment in our ten-part series (1/10) on Chirality is the perfect weekend morning read with your coffee. Chiral enthusiasts, enjoy this chiral treat! ☕✨

Asymmetric Synthesis and Biological Evaluation of Both Enantiomers of 5- and 6-Boronotryptophan as Potential Boron Delivery Agents for Boron Neutron Capture Therapy

To effectively utilize Boron Neutron Capture Therapy (BNCT), novel boron carriers must meet specific criteria, such as sufficient accumulation in tumor tissue, favorable ratios in blood and healthy tissue, and suitable pharmacokinetic properties. Current boron carriers fall short of these standards. This study developed new boronated tryptophan derivatives to efficiently deliver boron into tumor cells.

Chemists Invent Drugs and Drugs Save Lives

🌟✨ I believe this post, "Chemists Invent Drugs and Drugs Save Lives," will be the perfect way to close 2024 on a high note. Thank you all for your incredible support and engagement this year. See you in the NEW YEAR 2025!!! 🎉🥳 Let's continue to make great strides together! 🚀

2024 LinkedIn Unwrapped: The Year in Review!

Reflecting on the highlights, achievements, and moments that made this year unforgettable. Your support and engagement have been invaluable to my growth. Sharing insights and knowledge with you has been immensely rewarding. Here are a few of the standout posts that truly resonated with you this year.

The Future of Asymmetric Synthesis: Trends and Innovations

Excited to revisit our insightful blog post on "The Future of Asymmetric Synthesis: Trends and Innovations" originally featured on Chiralpedia! This marks the final installment in our five-part series on Asymmetric Synthesis.

Chiral Drugs Unleashed: Origins, Configuration, Pharmacology & Future Directions

Source: Shou-jiao Peng et al., Chiral drugs: Sources, absolute configuration identification, pharmacological applications, and future research trends. https://lnkd.in/gNwsaz-h

Revolutionary Leap: Rational Molecular Editing in Drug Discovery !

Here is a groundbreaking editorial: "Rational Molecular Editing: A New Paradigm in Drug Discovery".

Asymmetric Synthesis in Industry: From Lab to Market !

Rediscover the magic of "Asymmetric Synthesis in Industry: From Lab to Market"! This fourth installment in our five-part asymmetric synthesis series is a must-read for all chiral enthusiasts.

Explosive Breakthrough: Enantioselective Synthesis of (R)-Sitagliptin via Phase-Transfer Catalytic aza-Michael Addition!

Type 2 diabetes is a prevalent disease, and developing effective therapies is a key focus in drug discovery. Dipeptidyl peptidase IV (DPP-4) inhibitors, such as sitagliptin, elevate glucagon-like peptide-1 (GLP-1) levels to trigger insulin secretion and lower blood glucose. Approved by the FDA in 2006, sitagliptin has inspired many synthetic methods over the years. Approaches include chiral starting materials, auxiliaries, biocatalysis, organocatalysis, and transition-metal-based catalysis.

Synthesis and Clinical Application of New Drugs Approved by NMPA in 2023

In 2023, the NMPA approved 82 new therapeutic agents: 48 chemical drugs, 22 biological drugs, 4 vaccines, and 8 traditional Chinese medicines, focusing on oncology, CNS disorders, anti-infectives, hematology, cardiovascular diseases, ophthalmology, and immunomodulation.

Molecular Shape and Medicinal Chemistry: A Perspective - Shape Matters Like the Tune in a Symphony!

Drawing inspiration from Marcus Aurelius' timeless musings in "Meditations," this 2010 Perspective delves deep into the essence of molecules within medicinal chemistry. It captures the evolution of molecular descriptions and emphasizes the pivotal role of molecular shape in drug discovery. 🧬 While progress has been made in understanding properties like aromaticity and hydrophobicity, true advancement hinges on grasping the three-dimensional form. This work eloquently underscores the significance of molecular shape in predicting behavior, continuing to shape drug development... 💊

The Quinine Odyssey: A Barometer of the State of Organic Synthesis Over Centuries!

In 2024, we mark the 80th anniversary of Woodward and Doering's landmark synthesis of (±)-quinine, a millennium old chiral molecule.

Harnessing Computational Methods in Asymmetric Synthesis: Where Algorithms and Asymmetry Converge!

Thrilled to revisit our blog post on "Harnessing Computational Methods in Asymmetric Synthesis," originally created for Chiralpedia! This is the third installment in our five-part series on asymmetric synthesis.

Chiral Chemistry

I'm pleased to inform that I've been invited to share my thoughts and interact with the PG and Research Department of PSGR Krishnammal College for Women on "Chiral Chemistry". Looking forward to an enriching and insightful session! 🌟🔬

Recent Advances in Catalytic Asymmetric Synthesis

Thrilled to share our blog on "Recent Advances in Catalytic Asymmetric Synthesis," originally crafted for Chiralpedia! This is the second installment in our five-part series on asymmetric synthesis. Perfect time for a refreshing revisit with your Sunday morning coffee, chiral enthusiasts - Enjoy this enlightening Sunday treat ... !!! ☕🍵

Surface Molecularly Imprinted Biomimetic Magnetic Nanoparticles for Enantioseparation

A cost-effective, robust biomimetic magnetic nanomaterial for the separation of chiral drug molecules has been demonstrated. Using surface molecular imprinting, (S)-naproxen was imprinted on silica-coated iron oxide nanoparticles. The material showed high selectivity, binding capacity, and reusability, isolating (S)-naproxen effectively from its racemic mixture. This method offers a viable alternative to traditional chiral column separation techniques, with significant cost efficiency.

Revolutionary Catalysts: Unveiling the Power of Chiral Bicyclic Imidazoles in Modern Synthesis

Asymmetric organocatalysis is a key strategy for stereoselective preparation of optically active chemicals. Chiral tertiary amines as Lewis base organocatalysts have advanced various chemical transformations but face challenges in structural complexity and cost. To enhance activity and selectivity, new bicyclic imidazole catalysts were designed.

Understanding the Fundamentals of Asymmetric Synthesis.

Authored for Chiralpedia, sometime back.

Harnessing KRED: Scaling Up Enantiomerically Pure 3,4-Disubstituted Tetrahydrofuran

A scalable, eco-friendly synthesis of (3S,4S)-4-methyltetrahydrofuran-3-ol was achieved through a one-step biocatalytic reduction of a racemic ketone. This process, using keto reductase, operates under mild conditions with high enantio- and diastereoselectivity. The new route significantly improved key performance indicators, including PMI, solvent, and waste.

Chiral Switches: Still Alive and Kicking!

This perspective thoughtfully reexamines the enduring significance of classical chiral switches in pharmaceutical development. In contrast to a recent perspective, it delves into underexplored regulatory insights and emphasizes the synergistic effects observed in racemic drugs, exemplified by nebivolol. This nuanced perspective on chiral switches is an engaging and thought-provoking read.

Discovering Nitrogen Innovations: FDA-Approved Pharmaceuticals 2013-2023

This "perspective extends the analysis of U.S. FDA-approved small-molecule drugs containing nitrogen heterocycles from 1938–2012.

CHIRALITY: The Vital Role in Modern Drug Discovery

Source: Narmatha Senkuttuvan, et al., The significance of chirality in contemporary drug discovery-a mini review. https://lnkd.in/gNKfDCWf https://lnkd.in/g53PJHXQ

This article is sure to capture the interest of R&D Chemists and Engineers.

Advancing Chiral Chemistry: Organocatalytic Enantioselective Sulfur Alkylation of Sulfenamides for Sulfilimines Synthesis

In recent years, asymmetric synthetic methods for sulfur stereogenic centers have seen rapid development, significantly impacting drug discovery. Replacing carbon atoms with nitrogen in drug molecules has become a popular optimization strategy, as nitrogen can greatly enhance pharmacological properties. This is evident in the growing importance of chiral sulfoximines, the aza-analogs of sulfones. Nitrogen substitution at the sulfur center generates intrinsic chirality and provides additional modification sites. The nitrogen's lone pair also promotes favorable hydrogen bonding and coordination.

Recent Advances in Catalytic Desymmetrization for the Synthesis of Axially Chiral Biaryls

Atropisomeric compounds are important in pharmaceuticals and materials science. Their enantioselective synthesis has garnered significant attention. Desymmetrization is a robust method for creating axially chiral biaryls. It's simpler than other strategies due to easier substrate design. However, challenges like forming achiral products and distant reaction sites exist.

Advances on Greener Asymmetric Synthesis of Antiviral Drugs via Organocatalysis

Viral infections are a leading cause of severe human diseases and high mortality rates. This article underscores the critical efforts by academia and the pharmaceutical industry to discover new antiviral compounds.

Atropisomerism in the Pharmaceutically Relevant Realm

Atropisomerism, where there's restricted rotation around a bond leading to conformational chirality, is found in many drug structures like biaryls and heterobiaryls. These atropisomers vary in stability, with some being suitable for drug development.

Recent Advances in the Enantioselective Synthesis of Chiral Amines via Transition Metal-Catalyzed Asymmetric Hydrogenation

Chiral amines are crucial components found in many natural products, medicines, and biologically active substances. Over the past decade, significant progress has been made in creating chiral amines, especially through a process called catalytic asymmetric hydrogenation (AH).

Seven-membered N-heterocycles as approved drugs and promising leads in medicinal chemistry as well as the metal-free domino access to their scaffolds

Azepanes and azepines are key structures in numerous drugs, drug candidates, and tested lead compounds. Despite the frequent occurrence of N-heterocyclic 7-membered rings in nature, such as in alkaloids, naturally occurring compounds of this type are seldom approved as therapeutics.

Asymmetric Synthesis and Applications of Chiral Organoselenium Compounds: A Review

This paper reviews the development and application of organoselenium compounds, highlighting their significance in medicine, materials, and organic synthesis. It focuses particularly on chiral organoselenium compounds, essential for these fields. Despite their importance, producing these compounds in an ecofriendly manner remains a challenge.

Widened Scope of Drug Repurposing/Chiral Switches, Elements of Secondary Pharmaceuticals: The Quinine/Quinidine Case

This perspective article explores drug repurposing and chiral switches, focusing on the antimalarial quinine and the antiarrhythmic quinidine. It highlights how these drugs, with histories dating back to 1638, have been repurposed for new medical uses.

A Look at the Importance of Chirality in Drug Activity: Some Significative Examples

An excellent review that provides a brief overview of the most common chiral drugs used in therapy for treating various diseases.

Stereochemical diversity as a source of discovery in chemical biology

This review examines how chirality provides valuable chemical information at the chemistry-biology interface. It also looks at the chemical information density of FDA-approved drugs and the impact of stereochemistry on molecular complexity, with discussions on axial chirality and atroposelectivity as potential expansions.

Recent progress toward developing axial chirality bioactive compounds

Atropisomers are a special type of stereoisomers that have a unique kind of chirality due to restricted rotation around a single bond. Many of these axially chiral compounds have shown impressive biological activities, especially when targeting proteins. This dynamic form of chirality holds significant promise for developing new drugs.

The Quest for Secondary Pharmaceuticals: Drug Repurposing/Chiral-Switches Combination Strategy

This perspective introduces a new strategy that combines drug repurposing and chiral switches. It highlights examples like ketamine, flurbiprofen, fenfluramine, and milnacipran that has undergone this combination strategy. Also discusses a variation involving deuterium-enabled chiral switches of thalidomide analogs.

The Exploration of Chirality for Improved Druggability within the Human Kinome

This perspective explores how chirality can enhance the druggability of kinases, offering a valuable resource for developing innovative kinase inhibitors to meet current therapeutic needs.

Chiral Switch: Between Therapeutical Benefit and Marketing Strategy

This excellent review explores the evolution of the chiral switch concept over the past 25 years. Initially, it was believed that existing racemates would provide a rich source of new single enantiomer drugs, but this has proven challenging. However, in some cases, chiral switches have allowed racemate owners to extend their product lines, especially if marketed before the racemate’s patent expires.

Chirality: a key parameter in chemical probes

The article highlights how crucial it is to get chirality right in the pharmaceutical industry. Remember the thalidomide tragedy? It’s a stark reminder of what can go wrong when different isomers of a drug have different biological effects. The authors stress that developers and manufacturers need to be meticulous about chiral identity and purity to avoid wasting time and resources.

Asymmetric Synthesis of US-FDA Approved Drugs over Five Years (2016–2020): A Recapitulation of Chirality

An excellent review highlights the techniques used to synthesis FDA-approved chiral drugs from 2016 to 2020, focusing on asymmetric synthesis methods like chiral induction, resolution, and using chiral pools.

The future of Asymmetric Synthesis - Check out the 5th and last blog in this series.

I want to express my heartfelt appreciation to Dr. Gagan for his incredible efforts in writing concise overviews of excellent review papers published in reputed journals. By posting these summaries on LinkedIn, he is making these valuable papers more visible/accessible to the scientific community, especially to medicinal and organic chemists involved in drug design, discovery, and development. I truly understand the immense amount of time and dedication he puts into this task. In fact, he does this almost daily, like a ritual. Great job, Dr. Gagan!

Asymmetric Synthesis in Industry: From Lab to Market

Excited to share the 4th instalment in our blog series on Asymmetric Synthesis in Industry! Dive into how innovative strategies are transforming lab research into market-ready solutions. Perfect for professionals eager to bridge the gap between the lab bench and the commercial world.

Computational Methods in Asymmetric Synthesis!

Unveiling the Power of Computational Methods in Asymmetric Synthesis! 💻 Welcome back to our 5-part blog series on “Asymmetric Synthesis.” In this third instalment, we explore the transformative role of Computational Methods in Asymmetric Synthesis. 🌟

Recent Advances in Catalytic Asymmetric Synthesis

Happy to share that the 2nd part of our 5-part blog series on Recent Advances in Catalytic Asymmetric Synthesis🌟. In this, we delve deeper into the intricacies of asymmetric synthesis, exploring cutting-edge methodologies and novel catalysts that are pushing the boundaries of what's possible in this field. These advancements not only push the boundaries of what can be achieved in synthetic chemistry but also pave the way for groundbreaking applications in pharmaceuticals, agrochemicals, and beyond.

Understanding the Fundamentals of Asymmetric Synthesis

We're excited to launch a comprehensive 5-part blog series on "Asymmetric Synthesis." Dive into the world of asymmetric synthesis and discover the key concepts and techniques that drive innovation in pharmaceutical science. 💊🔬