Preparation of 2-Azabicyclo[2.1.1]hexane Hydrochloride

被引：10
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
收藏
页码：2251 / 2253
页数：3
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