摘要 |
PROBLEM TO BE SOLVED: To obtain a new compound having cyclooxygenase-2 which inhibits activity associated with the biosynthesis of prostaglandin E2 or the like, capable of exhibiting excellent antiinflammatory activity, improved water-solubility or the like, and useful as an antiinflammatory agent. SOLUTION: A compound of formula I (A1 and A2 are each CH= or N=; R1 is an alkyl or amine; R2 is aryl, a hetero cyclic group or the like; Q is O=, S= or the like; Y and Z are each H, an alkyl or the like), or its salt or hydrate, for example, (1-(4-fluorobenzyl)-5-methanesulfonylindol-2-yl)carbonylphrrolidine. In order to obtain a compound of formula I, for example, a new intermediate of formula III (R3 is an alkyl) is obtained by starting from a compound of formula II (RX is an alkyl; X is a halogen), and the obtained intermediate of formula III is treated, for example, with an amine having a group X and a group Z, or ammonia. The treatment with the amine or ammonia is preferably carried out at 20-40 deg.C by using methanol or the like as reaction solvent.
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