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3-(1-哌嗪基)-1,2-苯并异噻唑与(1R,2R)-1,2-双(甲磺酰基氧基甲基)环己烷在甲苯为溶剂、碳酸钾为碱、聚乙二醇400为相转移催化剂条件下反应得4’-(1,2-苯并异噻唑-3-基)-(3a R,7a R)-八氢螺-(2H-异吲哚-2,1’-哌嗪)甲磺酸盐,不经分离直接与顺-5-降冰片烷-外-2,3-二甲酰亚胺在碳酸钾为碱条件下反应制得鲁拉西酮,再在异丙醇中与盐酸成盐得盐酸鲁拉西酮,总收率达83%。该法收率高、操作简便,易于工业化生产。
(1R, 2R) -1,2-bis (methanesulfonyloxymethyl) cyclohexane in toluene as a solvent and potassium carbonate as a The reaction of 4 ’- (1,2-benzisothiazol-3-yl) - (3aR, 7aR) -octahydrospiro- 2’-piperazinyl) methanesulfonate, which was reacted directly with cis-5-norbornane-exo-2,3-dicarboximide without isolation in the presence of potassium carbonate as base Raloxifene, then salt with hydrochloric acid in isopropanol with Luludone hydrochloride, the total yield of 83%. The method of high yield, easy to operate, easy to industrial production.