Approach for synthesis of catechins

摘要

A process for synthesis of enatiomerically pure or enatiomerically enriched or racemic mixture of (+ and/or −) epicatechin and its intermediates, comprising the steps of: (i) obtaining penta-protected quercetin; (ii) reducing the penta-protected quercetin obtained from step (i); (iii) optionally deprotecting the compound of step (ii); (iv) reducing the compound obtained from step (ii) or step (iii) in the presence of a chiral/achiral reducing agent to obtain a chiral intermediate; (v) deprotecting and/or hydrogenation of the chiral intermediate obtained from step (iv) to obtain (−)-epicatechin; (vi) optionally simultaneously deprotecting and by drogenation of the compound obtained from step (ii) to obtain racemic epicatechin.

主权项

1. A process for synthesis of enatiomerically pure epicatechin, or enatiomerically enriched epicatechin, or a racemic mixture of (+) and (−) epicatechin, or its intermediates, comprising:
I. obtaining penta-protected quercetin in one or more than one selective protection steps; II. reducing the penta-protected quercetin obtained from step I; III. optionally deprotecting the compound of step II; IV. reducing the compound obtained from step II or step III in the presence of a chiral/achiral reducing agent to obtain a chiral intermediate; and V. deprotecting and/or hydrogenating the chiral intermediate obtained from step IV to obtain (−)-epicatechin; or VI. optionally simultaneously deprotecting and hydrogenating the compound obtained from step II to obtain racemic epicatechin.