337460-80-7Relevant academic research and scientific papers
Convenient efficient synthesis of TAK-779, a nonpeptide CCR5 antagonist: Development of preparation of various ammonium salts using trialkylphosphite and N-halogenosuccinimide
Ikemoto, Tomomi,Nishiguchi, Atsuko,Mitsudera, Hiroyuki,Wakimasu, Mitsuhiro,Tomimatsu, Kiminori
, p. 1525 - 1529 (2001)
A convenient and efficient synthesis of TAK-779 (1a), a nonpeptide CCR5 antagonist, has been achieved. The new methylation of tertiary amine (2) using trimethyl phosphite and N-chlorosuccinimide, followed by the addition of HCl led to ammonium chloride (1a) in 89% isolated yield without requiring a chromatographic method. By this preparation, ammonium methanesulfonate (1e) could be obtained in 75% isolated yield.
