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Part 10: Stereochemistry in Pharmaceutical Sciences – Current Trends and Future Directions

“Beyond today – emerging trends shaping the future of stereochemistry in pharma” Introduction The landscape of stereochemistry in pharmaceutical sciences continues to evolve with scientific and technological advances. This final part looks at emerging trends and future challenges. These include: – New developments in asymmetric catalysis, such as organocatalysts (MacMillan/List catalysts) that have expanded the toolkit for chiral synthesis, and the 2021 Nobel recognition of this field – implying more green and metal-free asymmetric processes …

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Part 9: Stereochemistry in Drug Discovery and Development

“From hit to lead to medicine – where stereochemistry shapes every stage of discovery” Introduction Stereochemistry is not only crucial in the final stages of drug production – it plays a significant role right from the discovery and lead optimization phases. In this part, we consider how medicinal chemists account for chirality when designing compounds and how structure-activity relationships (SAR) can depend on stereochemistry. We also look at how screening libraries incorporate stereochemical diversity, and …

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Ibuprofen

Ibuprofen is a widely used non-steroidal anti-inflammatory drug (NSAID). It is a monocarboxylic acid that is propionic acid in which one of the hydrogens at position 2 is substituted by a 4-(2-methylpropyl)phenyl group. Hence belongs to the propionic acid derivative class of NSAIDs. It is commonly prescribed for pain, inflammation, and fever. Available as over-the-counter (OTC) and prescription medication worldwide. Chirality and Biological Activity Structurally, Ibuprofen is a chiral molecule with one stereogenic center at the α-position …

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Part 7: Analytical Techniques for Stereochemistry

“Measuring handedness – tools and techniques that bring chirality into focus” Introduction Ensuring the correct stereochemistry and measuring stereochemical purity is a crucial aspect of pharmaceutical quality control and research. This part covers the major analytical techniques used to distinguish and quantify enantiomers and diastereomers in drug substances and products. Key techniques include: We’ll discuss how these techniques are applied in practice: e.g., during process development, a chiral HPLC method is developed to monitor enantiomeric …

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Part 5: Stereoselective and Stereospecific Synthesis

“Crafting molecules with precision – the art of stereochemical synthesis” Introduction Having seen why the correct stereochemistry is crucial for drug efficacy and safety, the next challenge is how to obtain the desired stereoisomer. This part covers strategies and methods in stereoselective and stereospecific synthesis. We clarify the terminology: a stereoselective reaction preferentially yields one stereoisomer over others (e.g., one enantiomer or one diastereomer is favored), whereas a stereospecific reaction produces different stereoisomeric products from …

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Part 1: Introduction to Stereochemistry

“The 3D language of molecules – why stereochemistry is the hidden key in drug science.” Introduction Stereochemistry is the branch of chemistry concerned with the three-dimensional arrangement of atoms in molecules and how this spatial arrangement influences chemical behavior. The term “chirality” (from the Greek cheir meaning hand) describes the property of an object or molecule that is non-superimposable on its mirror image – much like one’s left and right hands. A molecule that exhibits …

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Chiral Bioequivalence – An Explainer  

Introduction Chirality, or “handedness,” is the unique property of molecules that exist as non-superimposable mirror images, known as enantiomers. Drugs that exhibit handedness are referred to as chiral drugs. Chiral medications consisting of an equal (1:1) mixture of enantiomers are called Racemic drugs. In drug development, chirality is incredibly important because most biological molecules, like enzymes and receptors, are chiral. This characteristic affects how a drug interacts with biological targets, leading to significant differences in …

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Chiral Switch: Unlocking the Potential of Single Enantiomers

Synopsis Welcome to an exploration of Chiral Switch!!! Chiral switching revolutionizes the pharmaceutical landscape by transforming racemic drugs into their more effective single-enantiomer forms, enhancing therapeutic efficacy and reducing side effects This blog post delves into the intriguing realm of chiral switches, presenting key concepts such as chiral switch strategies, their advantages, and the regulatory environment focusing on bridging studies. An engaging mind map highlights notable case studies, both successful and unsuccessful, and also examines …

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Chiral Drugs: A twisted tale in pharmaceuticals

Synopsis Chiral drugs, those fascinating chemical compounds existing as mirror-image pairs or enantiomers, exhibit distinct biological properties. This post provides a comprehensive overview of chiral drugs, presenting key concepts through a visually engaging mind maps. It covers chirality’s historical roots and stereochemical nomenclature, delves into the specialized discipline of chiral pharmacology, and presents drug toxicity case studies. Additionally, it explores unichiral drugs, the importance of chiral purity, and the tools used for measuring it. Designed …

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The Future of Asymmetric Synthesis: Trends and Innovations”

Introduction Asymmetric synthesis has made significant strides in recent decades, becoming a crucial component of pharmaceutical, agrochemical, and fine chemical industries. The development of chiral catalysts and the understanding of stereoselective reactions have enabled the production of enantiomerically pure compounds on an industrial scale. This blog explores the future perspectives in chiral asymmetric synthesis, focusing on emerging technologies, interdisciplinary approaches, global impact, and the challenges that lie ahead. Emerging Technologies Green Chemistry Approaches The future …

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