Small molecule drug discovery chiral drugs

There are two main approaches to discovering small molecule drugs the irrational approach or the more recent structured rational approach. Antisense, RNA interference, and chiral drugs are other drug discovery methodologies. 

During drug discovery, screening and candidate optimization, an expedient approach to target molecules is preferred to prepare small amounts of material for rapid assessment of in vitro activity. Accordingly, the initial preparation of 50 g of our drug candidate relied upon a direct adaptation of a literature procedure that employed a chiral auxiliary (Fig. 2) [3]. 

Because the priority during the first phase of drug discovery is rapid access to target molecules, the use of chiral reagents and chiral catalysts is fairly uncommon, with successful applications confined to a small number of well developed methodologies. Pre-eminent amongst these is the Sharpless epoxidation of allylic alcohols, which was first reported as a stoichiometric method in 1980 [105] and later adapted into a practical catalytic variant [106]. 

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