Abstract
In the past decade there has been a significant growth in the sales of pharmaceutical drugs worldwide, but more importantly there has been a dramatic growth in the sales of single enantiomer drugs. The pharmaceutical industry has a rising demand for chiral intermediates and research reagents because of the continuing imperative to improve drug efficacy. This in turn impacts on researchers involved in preclinical discovery work. Besides traditional chiral pool and resolution of racemates as sources of chiral building blocks, many new synthetic methods including a great variety of catalytic reactions have been developed which facilitate the production of complex chiral drug candidates for clinical trials. The most ambitious technique is to synthesise homochiral compounds from non-chiral starting materials using chiral metal catalysts and related chemistry. Examples of the synthesis of chiral building blocks from achiral materials utilizing asymmetric hydrogenation and asymmetric epoxidation are presented.
Highlights
Chiral chemical synthesis plays an important and growing role in the development of new drugs, agrochemicals and building blocks
This paper focusses on asymmetric synthesis with chiral catalysts to provide novel chiral amino acids and amino alcohols
Chiral catalysis has proven an effective means of preparing key chiral intermediates in high ee
Summary
Chiral chemical synthesis plays an important and growing role in the development of new drugs, agrochemicals and building blocks. The reaction mixture was allowed to reflux overnight cooled to room temperature and the solvent removed to give amino methyl ester 10 as a yellow powder (8.1 g, 89% yield). The organic layer was dried over sodium sulfate, filtered and concentrated to afford a white solid (2.09 g) which was taken up in 3 N hydrochloric acid and lyophilised to provide (S)-amino alcohol 16 as a pale yellow solid (1.99 g, 81% yield).
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