Efficient synthesis of [6-chloro-2-(4-chlorobenzoyl)-1H-indol-3-yl]-acetic acid,a novel COX-2 inhibitor |
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Authors: | Caron Stéphane Vazquez Enrique Stevens Rodney W Nakao Kazunari Koike Hiroki Murata Yoshinori |
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Institution: | Chemical R&D, Pfizer Global Research & Development, Groton, Connecticut 06340-8118, USA. stephane_caron@groton.pfizer.com |
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Abstract: | The synthesis of 6-chloro-2-(4-chlorobenzoyl)-1H-indol-3-ylacetic acid (1), a selective cyclooxygenase 2 (COX-2) inhibitor, is described. The synthesis relied on a novel indole formation that involved an alkylation/1,4-addition/elimination/isomerization cascade. It was demonstrated that the entire sequence from sulfonamide 13 and bromoketone 14 to the desired indole (1) could be executed in a single pot. |
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