A Facile Route to Functionalized Cyclopenta[b]thiophenones Based on the Structure of the Selective COX-2 Inhibitor Flosulide

摘要: The synthesis of three thiophene analogues Flosulide – a potent and selective inhibitor cyclooxygenase subtype 2 (COX-2) is described. Utilizing combined Friedel-Crafts acylation alkylation 2-chlorothiophene, simplified procedures were developed to obtain cyclopenta[b]- thiophenones as key products which further derivatized by nitration, nucleophilic aromatic substitution, reduction, mesylation.