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向tubulysin 迈进:tubuvaline-tubuphenylalanine 片段的克级合成。

Toward tubulysin: gram-scale synthesis of tubuvaline-tubuphenylalanine fragment.

机构信息

Organic Division-I, Indian Institute of Chemical Technology, Hyderabad 500 607, India.

出版信息

J Org Chem. 2009 Dec 18;74(24):9531-4. doi: 10.1021/jo9015503.

Abstract

A practical and stereoselective synthesis of the tubuvaline-tubuphenylalanine (Tuv-Tup) fragment of tubulysin is achieved involving the opening of aziridine, crucial MacMillan alpha-hydroxylation on both fragments, and an epoxide-opening reaction.

摘要

实现了tubulysin 中tubuvaline-tubuphenylalanine(Tuv-Tup)片段的实用和立体选择性合成,涉及氮丙啶的开环、两个片段的关键 MacMillan α-羟化作用以及环氧化物开环反应。

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