Buchwald-Hartwig (B-H) amination reaction is a powerful method for the catalytic C-N bond formation, which has found numerous applications recently in the construction of Active Pharmaceutical Ingredient (API) in pharmaceutical industry. A recent case study is discussed herein. This presentation focuses on the process optimization and development of the B-H amination of a highly functionalized 2-chloropyridine substrate and a 4-aminopyridine substrate to form a key C-N bond in the API. Development work on the work-up (including Pd depletion) and controlled crystallization is also described. The optimized process conditions successfully produced multi-kg material.

Process development of a Buchwald-Hartwig amination

256th National Meeting (2018)

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