申请人:Asahi Kasei Kabushiki Kaisha
公开号:EP1209150A1
公开(公告)日:2002-05-29
A process for the preparation of tricyclic amino alcohol derivatives including 2-[N-[2-(9H-carbazol-2-yloxy)ethyl]]amino-1-[(3-methylsulfonylamino)phenyl]ethanol useful in the treatment of diabetes, obesity, hyperlipidemia and so on; and intermediates as represented by formula (5) or (6) or the like useful in the preparation, wherein R11 is hydrogen or the like; and *1 represents an asymmetric carbon atom. 2-Halo-1-(3-nitrophenyl)ethanone derivatives and 1-(3-nitrophenyl)oxirane derivatives, which are intermediates for the preparation of tricyclic amino alcohol derivatives, are easy of purification, and particularly optically active 1-(3-nitrophenyl)oxirane derivatives are effective in enhancing the optical purities of the final products.
一种制备三环氨基醇衍生物的工艺,包括用于治疗糖尿病、肥胖症、高脂血症等的2-[N-[2-(9H-咔唑-2-氧基)乙基]]氨基-1-[(3-甲磺酰氨基)苯基]乙醇;以及用于制备的式(5)或式(6)或类似物所代表的中间体,其中R11为氢或类似物;*1代表不对称碳原子。2-Halo-1-(3-nitrophenyl)ethanone 衍生物和 1-(3-硝基苯基)环氧乙烷衍生物是制备三环氨基醇衍生物的中间体,易于纯化,特别是具有光学活性的 1-(3-硝基苯基)环氧乙烷衍生物可有效提高最终产品的光学纯度。