Michael J. Schmitt

Intramolekulare [3+2]-cycloadditionen von azoxygruppen mit benachbarten olefineinheiten

Abstract The azoxy compounds 4 , easily obtained from 1 , undergo intramolecular [3+2]-cycloaddition thermally or acid catalyzed forming the stable 1,2,3-oxadiazolidines 5 .

Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.

We have previously reported that optimization of a series of phenylacetic acid derivatives led to the discovery of CRTH2 and DP dual antagonists, such as AMG 009 and AMG 853. During the optimization process, we discovered that minor structural modifications also afforded potent and selective CRTH2 or DP antagonists. Here we report the structure-activity relationship that led to the discovery of selective CRTH2 antagonists such as 2 and 17, and selective DP antagonists, such as 4 and 5.