关键词: 塞来昔布, 合成, 工艺优化, 塞来昔布, 合成, 工艺优化

Abstract: Celecoxib is the first selective COX-2 inhibitor of non-steroidal anti-inflammatory drugs，it mainly inhibit COX-2 enzyme protein which is necessary for prostaglandin biosynthesis process to achieve anti-inflammatory effects. Its side effects are much smaller than that of traditional anti-inflammatory drugs. Its analgesic anti-inflammatory activity is of great research value and broad application prospects. Since going public，Celebrex has been one of the world’s best selling drugs. In recent years，a growing domestic demand for celebrex and more attention has been paid to its good development prospect. The compound patent delay （reissue） expires in 2015. There are many reports on the synthesis of celecoxib at home and abroad. It is aimed at the synthesis progress of celecoxib by different reaction mechanism，such as dehydration，cyclization，cycloaddition，coupling，Michael addition，catalysis and arylation. We analyzed the traditional two-step preparation process of celecoxib by ester condensation and dehydration cyclization and its optimization process. It is concluded that the traditional method by dehydration cyclization is moderate and stable. It’s also suitable for industrialized production. The regional isomer impurity during the reaction can be removed by suitable recrystallization solvent. What’s more，the celecoxib we prepared can reach the national drug standards.

Key words: Celecoxib, synthesis, process optimization