Abstract
EP4 Receptor antagonists are candidates for the treatment of inflammatory disorders associated with arachidonic acid metabolism. Noteworthy steps in the synthesis shown were (1) a large-scale Kulinkovich cyclopropanation (A → B), (2) an FeCl3-catalyzed Friedel-Crafts benzylation of 2,5-dimethylthiophene (E) using 4-trifluoromethylbenzyl alcohol (D) as the electrophile and (3) an FeCl3-catalyzed Friedel-Crafts acylation of thiophene F using isocyanate C as the electrophile.
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