Title of article
A convergent approach to the synthesis of aprepitant: a potent human NK-1 receptor antagonist
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 ,
Issue Information
هفته نامه با شماره پیاپی سال 2007
Pages
4
From page
8001
To page
8004
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.
Journal title
Tetrahedron Letters
Serial Year
2007
Journal title
Tetrahedron Letters
Record number
1857174
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