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通过铑/二烯催化的 1,4-加成反应进行β-取代γ-内酰胺的不对称合成:在(R)-巴氯芬和(R)-罗利普兰合成中的应用。

Asymmetric synthesis of β-substituted γ-lactams via rhodium/diene-catalyzed 1,4-additions: application to the synthesis of (R)-baclofen and (R)-rolipram.

机构信息

Key Laboratory of Synthetic Chemistry of Natural Substances, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China.

出版信息

Org Lett. 2011 Feb 18;13(4):788-91. doi: 10.1021/ol103054a. Epub 2011 Jan 19.

Abstract

An efficient rhodium/diene-catalyzed asymmetric addition of arylboronic acids to α,β-unsaturated γ-lactams has been developed. The power of this methodology is further demonstrated by the concise synthesis of (R)-baclofen and (R)-rolipram.

摘要

一种高效的铑/二烯催化的芳基硼酸对α,β-不饱和γ-内酰胺的不对称加成反应已经被开发出来。该方法的强大之处还通过(R)-巴氯芬和(R)-罗利普兰的简洁合发展得到了进一步证明。

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