Advanced Practical Medicinal Chemistry by Ashutosh Kar

By Ashutosh Kar

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In short, synthetic medicinal chemistry, with the skill, wisdom and effort, has proved to be a major endeavor not only confined to the laboratories of Universities in general, but also to the bulk-drug industry in particular. 2. CONCEPTUALIZATION OF A SYNTHESIS In the past one century and a half ‘research chemists’ across the globe have evolved an innumerable, viable and potential synthetic routes for the preparation of any conceptualized ‘target-drug-molecule’. Interestingly, in the last four decades or so the very emergence of 15 P-IV\C:\N-ADV\CH2-1 16 ADVANCED PRACTICAL MEDICINAL CHEMISTRY the creation of piecing together a logical-philosophy and a well-conceived theoretical design have, in fact, made the entire task of complicated and strategic ‘drug-design’ into a rather easier and viable proposition.

Paradoxically, one may expect a, pure and reasonably good desired ‘target-drug-molecule’ if and only when one makes use of pure starting materials ; of course, under rigid experimental conditions. Salient Features of Materials. Following are some of the generalized salient features of starting materials, such as : (1) Chemical compounds bearing simple-linear skeletons essentially having one to six carbon atoms and one functional moiety are available commonly. Such compounds generally give rise to certain basic organic entities, for instance : aldehydes, ketones, carboxylic acids and their derivatives, alcohols, and organohalogens.

P-IV\C:\N-ADV\CH2-2 41 DRUG SYNTHESIS Explanation. The HI liberated from NaOH/I2 is added onto the prevailing double bond of cyclohexen-3-ene carboxylic acid (I), thereby affording an intramolecular addition, usually termed as iodolactonization. 3 Catalytic Hydrogenations Generally, the catalytic hydrogenation are nothing but syn-additions*. However, these reactions are able to be relied on as stereospecific in proceeding from the less-hindered side of the molecule. In instances, when the double bond is strategically located in a ring, the reaction involved is invariably anti-addition** because it is ‘anti’ to the main bulkiest substitutent.

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