Dj. Reynolds et Sa. Hermitage, The synthesis of GW710936X to support the development of potent PPAR gammaagonists, TETRAHEDRON, 57(36), 2001, pp. 7765-7770
(2S)-[(2-Benzoyl-4-hydroxy-phenyl)amino]-3-{4-[2-(5-methyl-2-phenyloxazol-4
-yl)ethoxy]pheny}propanoic acid has been synthesised from N-Cbz-L-tyrosine
methyl ester utilising a copper(I) catalysed N-arylation as the key couplin
g step. The synthetic route was designed to be convergent and to facilitate
ease of isolation of the unstable product that had proven to be unobtainab
le by concentration of extracts from biological assays. (C) 2001 Elsevier S
cience Ltd. All rights reserved.