1141997-95-6Relevant academic research and scientific papers
Development and large-scale preparation of an oral TACE inhibitor
Savage, Scott A.,Waltermire, Robert E.,Campagna, Silvio,Bordawekar, Shailendra,Toma, Joan Dalla Riva
experimental part, p. 510 - 518 (2010/04/22)
An efficient, expedient synthesis of BMS-561392, 1, which enabled rapid delivery of drug substance for clinical development is described. The key features of the synthesis include an efficient synthesis of a phenolic α,α-disubstituted amino ester via carbon alkylation without protection of the phenol, an effective enzymatic resolution of this racemic amino ester, and a process for the preparation of a hydroxamic acid drug substance with undetectable levels of hydroxylamine.
