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(+)-L-733,060、(+)-CP-99,994 和 (2S,3R)-3-羟基哌啶酸的合成:有机催化直接维替尼奥尔缩合反应的应用。

Synthesis of (+)-L-733,060, (+)-CP-99,994 and (2S,3R)-3-hydroxypipecolic acid: application of an organocatalytic direct vinylogous aldol reaction.

机构信息

Department of Chemistry, Memorial University, St. John's, Newfoundland, Canada, A1B 3X7.

出版信息

Org Biomol Chem. 2012 Mar 14;10(10):2119-25. doi: 10.1039/c2ob06644k. Epub 2012 Jan 31.

DOI:10.1039/c2ob06644k
PMID:22294285
Abstract

The γ-butenolide obtained from an organocatalyzed, direct vinylogous aldol reaction of γ-crotonolactone and benzaldehyde serves as the key starting material in the expedient synthesis of a 3-hydroxy-2-phenyl piperidine intermediate which is converted to the target 2,3-disubstituted piperidines.

摘要

由γ-丁烯内酯与苯甲醛经有机催化的直接 vinylogous aldol 反应得到的γ-丁内酯是一种关键的起始原料,用于快速合成 3-羟基-2-苯基哌啶中间体,然后将其转化为目标 2,3-二取代哌啶。

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