Organic Process Research and Development p. 2378 - 2387 (2019)
Update date:2022-07-31
Topics:
Hirasawa, Shun
Kikuchi, Takashi
Kawazoe, Souichirou
ASP3627 (1) is a potent Janus kinase inhibitor discovered and developed by Astellas Pharma Inc. Here, we report the development of a practical and scalable method for manufacturing ASP3627 featuring a six-reaction telescoping process consisting of DIBAL reduction, hydrolysis, Wittig reaction, cyclization, and a two-step sequence to remove the SEM group. In addition, a simple palladium removal procedure using l-cysteine is described. This method was used to successfully perform the first multikilogram synthesis of ASP3627, producing 30 kg with high purity in excellent overall yield.
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Doi:10.1002/chem.201000429
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