878809-88-2Relevant articles and documents
Development of a Multikilogram Scale Synthesis of a TRPV1 Antagonist
Kuethe, Jeffrey T.,Journet, Michel,Peng, Zhihui,Zhao, Dalian,McKeown, Arlene,Humphrey, Guy R.
, p. 227 - 232 (2016/03/04)
A highly efficient, regioselective five-step synthesis of the TRPV1 antagonist 1 is described. The coupling of piperazine 7 with dichloropyrimidine 8 proceeded via a regioselective Pd-mediated amination affording product 11 in excellent yield. Conversion of the penultimate product 14 afforded 1 through formation of a magnesium ate complex and trapping with CO2.