Synthesis and Structural Analysis of a New Class of Azaspiro[3.3]heptanes as Building Blocks for Medicinal Chemistry

被引：96

作者：

Burkhard, Johannes A. ^{[1
]}

Guerot, Carine ^{[1
,2
]}

Knust, Henner ^{[2
]}

Rogers-Evans, Mark ^{[2
]}

Carreira, Erick M. ^{[1
]}

机构：

[1] ETH, Organ Chem Lab, CH-8093 Zurich, Switzerland

[2] F Hoffmann La Roche & Cie AG, Discovery Chem, CH-4070 Basel, Switzerland

来源：

ORGANIC LETTERS | 2010年 / 12卷 / 09期

关键词：

AMIDE GROUP; OXETANES; 1,3,3-TRINITROAZETIDINE; DIETHOXYTRIPHENYLPHOSPHORANE; STEREOCHEMISTRY;

D O I：

10.1021/ol1003302

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Straightforward access toward previously unreported substituted, heterocyclic spiro[3.3]heptanes is disclosed. These spirocyclic systems may be considered as alternatives to 1,3-heteroatom-substituted cyclohexanes, which are otherwise insufficiently stable to allow their use in drug discovery. Conformational details are discussed on the basis of X-ray crystallographic structures.

引用

页码：1944 / 1947

页数：4

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