伊潘立酮的合成与表征

目的：为了探索一种合成伊潘立酮的新方法。方法：以4-（2，4-二氟苯甲酰基）哌啶盐酸盐为原料，经肟化、环合反应生成6-氟-3-（哌啶-4-基）-1，2-苯并异嗯唑，然后与4-（3-氯丙氧基）-3-甲氧基苯乙酮在碳酸钾存在下发生N-烷基化反应制得伊潘立酮。结果：探索出一个合成伊潘立酮的新方法，总收率53．29／5，化合物结构经。HNMR和13CNMR表征。结论：合成路线总收率高，操作简便，条件温和。

Synthesis and characterization of iloperidone

Objective. To investigate a new synthetic method of iloperidone. Methods. Using（2,4-di fluorophenyl） 4-yl-piperidine hydrochloride as the starting material, 6-fluoro-3-（piperidin-4-yl）-1,2 benzisoxzole was obtained by reactions of oximination and cyclization. Then, the N-alkylation of in termediate was performed to produce the desired 4-（3-chloropropoxy）-3-methoxy-phenylethanone in the presence of potassium carbonate. Results： A new method for the synthesis of iloperidone has been found with an overall yield of about 53.2%. The structures of all compounds were represented bylH NMR and 13C NMR. Conclusion. The synthetic process features high yield, simplicity in op eration, mild reaction conditions.