Development of an Optimized Process for the Preparation of 1-Benzylazetidin-3-ol: An Industrially Important Intermediate for Substituted Azetidine

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• 作者：V. V. R. M. Krishna Reddy ; D. Udaykiran ; U.S. Chintamani ; E. Mahesh Reddy ; Ch. Kameswararao ; G. Madhusudhan
• 刊名：Organic Process Research & Development
• 出版年：2011
• 出版时间：March 18, 2011
• 年：2011
• 卷：15
• 期：2
• 页码：462-466
• 全文大小：721K
• 年卷期：v.15,no.2(March 18, 2011)
• ISSN：1520-586X

文摘

A thoroughly optimized and robust process for the synthesis of 1-benzylazetidin-3-ol has been emphasized. 1-Benzylazetidin-3-ol has been utilized as a starting material in the commercial synthesis of azetidin-3-ol hydrochloride. Synthesis of azetidin-3-ol hydrochloride involves the usage of very low cost and commercially available starting material (benzylamine) and with reduced formation of di(3-chloro-2-hydroxypropyl) benzylamine significantly resulting in an economical process that allows the effective production of 1-benzyl azetidin-3-ol as well as azetidin-3-ol hydrochloride.