Preparation of 2-Azabicyclo[2.1.1]hexane Hydrochloride

被引：11

作者：

Liao, Haili ^{[1
]}

Li, Aimin ^{[1
]}

Chen, Xingsong ^{[1
]}

Liang, Kun ^{[1
]}

Shen, Yang ^{[1
]}

Liang, Qingfeng ^{[1
]}

Xu, Kewei ^{[2
]}

Shore, Daniel G. M. ^{[2
]}

Villemure, Elisia ^{[2
]}

Siu, Michael ^{[2
]}

Huestis, Malcolm P. ^{[2
]}

机构：

[1] Pharmaron Beijing Co Ltd, BDA, 6 Taihe Rd, Beijing 100176, Peoples R China

[2] Genentech Inc, Discovery Chem, 1 DNA Way, San Francisco, CA 94080 USA

来源：

SYNLETT | 2016年 / 27卷 / 15期

关键词：

amines; alkylation; alkyl halides; bicyclic compounds; heterocycles; 2,4-METHANOPROLINE; DIVERSITY;

D O I：

10.1055/s-0035-1562380

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A batchwise, multigram preparation of 2-azabicyclo-[2.1.1]hexane hydrochloride (1<bold>HCl</bold>) was developed, delivering a total of 195 grams of material. The key synthetic step involves an intramolecular displacement of a primary alkyl chloride with a tert-butylsulfinamide to forge the [2.1.1]-bicyclic ring system.

引用

页码：2251 / 2253

页数：3

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