4.6 Article

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

Journal

ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 15, Issue 2, Pages 462-466

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/op100247m

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Funding

  1. Inogent Laboratories Private Limited (A GVK BIO Company)

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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 azeticlin-3-ol as well as azetidin-3-ol hydrochloride.

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