格列美脲的制备工艺研究

Studies on the Preparation of Glimepiride

对格列美脲及其中间体的制备进行了研究。合成工艺：3-乙基-4-甲基-3-吡咯啉-2-酮与B-苯乙基异氰酸酯在甲苯中缩合，所得产物与氯磺酸以1：5（物质的量比）的比例磺化，然后在30—45℃氨解，最后与反-对甲基环己基异氰酸酯在丙酮中合成格列美脲。精制工艺：苯磺酰胺：95％乙醇重结晶；格列美脲：甲醇氨-甲醇重结晶。总收率达到39．4％。

Studied the preparation of glimepiride and its intermediates. Synthesis： the condensation substance of 3 - ethyl - 4 - methyl - pyrrolin - 2 - one with 13 - phenylethyl isocyanate in toluene was sulfonated by chlorosulfonic acid in 1：5 （ molar ratio）, then was ammoniated in 30 - 45℃. Finally glimepiride was synthesized via condensation of benzyl -sulphonamide substance with trans- 4 -methycyclohexyl isocyanate in acetone. Refining： benzyl- sulphonamide substance, recryetaUization in 95% ethanol,rlimepiride,recryctallization in ammonia methoxide - methanol. The total yield increased to 39.4%.