Improved Process for the Preparation of 1-Benzhydrylazetidin-3-ol: Development of an Efficient Synthesis and Identification of Process-related Impurities and/or Intermediates

摘要

An improved, one-pot, and multikilogram-scale synthesis of l-benzhydrylazetidin-3-ol, the pharmaceutically important moiety, has been developed. The improved process for the preparation of l-benzhydrylazetidin-3-ol was able to minimize a content of impurities and allows the effective production of 1-benzhydry-lazetidin-3-ol and its scale-up. The process was high yielding (80%) and chromatography-free with purity 99.3 area %.