By Ashutosh Kar
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Extra resources for Advanced Practical Medicinal Chemistry
From a close-look of the target-drug-molecule the researcher may logically ponder over the ways and means to accomplish their objective through the kinds of reaction(s) to make use in a sequential manner. In other words, the strategic attack on the target-drug-molecule may be conveniently and formally divided into two major components, namely : (a) Basic Carbon Skeleton. The importance of the basic carbon skeleton present in the conceived and proposed target-drug-molecule structure in any synthesis, cannot be ruled out.
In other words, the former enjoys its existence and importance to build up desired C—C skeletons and, therefore, are absolutely necessary in a synthesis ; however, the latter causes degradation or split-up of C—C skeletons and they also possess certain vital synthetic utility. There are, in fact, two important reactions that are particularly useful in affording the fragmentation reactions, such as : (i) Ozonolysis, and (ii) Decarboxylation reaction. 1 Ozonolysis. Ozonolysis (cleavage by ozone ‘O3’) is accomplished in two stages, namely : first, addition of ozone to the double bond to form an ozonide ; and secondly, subsequent hydrolysis of the ozonide to produce the cleaved products.
P-IV\C:\N-ADV\CH2-1 20 ADVANCED PRACTICAL MEDICINAL CHEMISTRY (3) Aromatic compounds that are available readily include : most of the benzene structural analogues having essentially either one or two functional groups attached ; besides, having side-chains consisting of upto 4 C-atoms with one functional moiety. (4) Optically active chiral molecules that are available mostly belong to natural sources, namely : simple sugars, terpenes, and amino acids. Broadly speaking, a research chemist profusely utilizes his wisdom and skill in designing the synthesis of rather complex natural products by employing relatively small synthons comprising of 1 to 5 C-atoms.