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Retrosynthesis in the Manufacture of Generic Drugs: Selected Case Studies (en Inglés)
Pedro Paulo Santos; William Heggie (Autor)
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· Tapa Dura
Retrosynthesis in the Manufacture of Generic Drugs: Selected Case Studies (en Inglés) - Pedro Paulo Santos; William Heggie
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Origen: Estados Unidos
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Reseña del libro "Retrosynthesis in the Manufacture of Generic Drugs: Selected Case Studies (en Inglés)"
This book illustrates how the retrosynthetic tool, widely used by academics in the search for synthetic routes used to prepare novel organic compounds, is applied in the Pharmaceutical Industry. However, merely finding a viable synthetic route is not sufficient. Many different options have to be considered and evaluated, as there exist numerous constraints on the industrialist in terms of what can and what cannot be reduced to practice. The reader will be guided through the various steps leading to the "best" processes and the limits encountered if these are put into practise on an industrial scale of seven key Active Pharmaceutical Ingredient (API). Thereafter, an evaluation the potential each process has for implementation is presented. It merges the two points of view, of retrosynthesis, and process chemistry, showing how retrosynthetic analysis is helpful in selecting the most efficient route for an industrial synthesis of a particular compound whilst giving insight into the industrial process per se. Some key concepts used by process chemists to improve efficiency (e.g. convergent/linear routes, placement of a low yield step) are used to indicate the best route to select, as most of these factors are not usually considered by academic organic chemists. One chapter is dedicated to each drug, with each containing the following information: 1) Worldwide sales and patent status of the Active Pharmaceutical Ingredient (API) 2) Structure analysis and general retrosynthetic strategy of the API (main features and challenges for the chemist) 3) First reported synthesis 4) Critical analysis of the processes which have been developed and. comparison of the synthetic routes. 5) Lessons learned (key ideas to be retained that can be applied for other molecules and situations) 6) Reaction conditions for Schemes A to X 7) Chemical "highlights" on key reactions used during the synthesis 8) References A unique feature of this book is the use of "reaction maps" (likened to underground/metro maps) which display several synthetic processes in the same scheme. The reaction maps allow easy comparison of the different routes which give the same molecule or intermediate.
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