Author/Authors :
Elati، نويسنده , , Chandrashekar R. and Kolla، نويسنده , , Naveenkumar and Gangula، نويسنده , , Srinivas and Naredla، نويسنده , , Anitha and Vankawala، نويسنده , , Pravinchandra J. and Avinigiri، نويسنده , , Muttu L. and Chalamala، نويسنده , , Subrahmanyeswararao and Sundaram، نويسنده , , Venkatraman and Mathad، نويسنده , , Vijayavitthal T. and Bhattacharya، نويسنده , , Ap، نويسنده ,
Abstract :
A simple and convergent approach to enantiomerically pure 5-[[2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one 1, a potent orally active antagonist of the human neurokinin-1 (NK-1) receptor, is described. The synthetic procedure starts from p-fluorobenzaldehyde to access the racemic morpholinone 2 via a modified Strecker synthesis and utilizes a diastereomeric salt resolution technique to accomplish the synthesis of 1 in enantiomerically pure form and good yield.
