首页> 外国专利> A PROCESS FOR THE PREPARATION OF (-) 3R, 4R-TRANS-2,2-DIALKYL-3-SUBSTITUTED PHENYL-4-(HYDROXY-SUBSTITUTED PHENYL)-SUBSTITUTED CHROMANS

A PROCESS FOR THE PREPARATION OF (-) 3R, 4R-TRANS-2,2-DIALKYL-3-SUBSTITUTED PHENYL-4-(HYDROXY-SUBSTITUTED PHENYL)-SUBSTITUTED CHROMANS

机译:制备(-)3R,4R-TRANS-2,2-二烷基-3-取代的苯基-4-(羟基取代的苯基)取代的铬的方法

摘要

This invention relates to a process for the preparation of (-) 3R, 4R - trans -2,2-dialkyl -3- substituted phenyl-4- (hydroxy substituted phenyl)- substituted chromans. The product is used as key intermediates for the preparation of tissue selective estrogens as pharmaceuticals. The product of the structure 2, where in R1 and R4 are individually hydrogen, hydroxy, halogens, C1-6 alkyl, C1-6 alkoxy, R2, R3, are individually hydrogen, C1-6 alkyl and R5 is hydrogen, halogen, nitro, cyano, C1-6 alkyl or cyclic alkyloxy, is prepared by treating 3R, 4R- trans - 2,2-dialkyl -3- substituted phenyl-4-(ω-aminoalkoxy substituted phenyl)- substituted chroman derivatives of structure 3 where in R1, R2, R3, R4 and R5 are as stated above and R6 is a methyl iodide salt of a substituted amino alkoxy group, with an inorganic base 3R, 4R- trans - 2,2-dialkyl -3- substituted phenyl-4- of formula 3 with inorganic base, , isolating the hydroxide salt and reacting the isolated hydroxide salt with cyclic amines in a high boiling solvent at a temperature in the range of 80°C to 200°C for a period of 5 minutes to 8 hrs or insitu conversion of methyliodide salt to desired compound of structure 2 using above stated methodology.
机译:本发明涉及一种制备(-)3R,4R-反--2,2-二烷基-3-取代的苯基-4-(羟基取代的苯基)-取代的苯并二氢吡喃的方法。该产品用作制备药物的组织选择性雌激素的关键中间体。结构2的产物,其中在R 1和R 4中分别为氢,羟基,卤素,C 1-6烷基,C 1-6烷氧基,R 2,R 3分别为氢,C 1-6烷基且R 5为氢,卤素,硝基氰基,C 1-6烷基或环状烷氧基是通过处理结构的3R,4R-反式-2,2-二烷基-3-取代的苯基-4-(ω-氨基烷氧基取代的苯基)-取代的苯并二氢吡喃衍生物而制备的3其中R 1,R 2,R 3,R 4和R 5如前所述,R 6是取代的氨基烷氧基的甲基碘盐,具有3R,4R-反式-2,2-二烷基-3-取代的无机碱式3的-4-与无机碱的反应,分离氢氧化物盐并使分离的氢氧化物盐与环胺在高沸点溶剂中在80℃至200℃的温度下反应5分钟。 8小时或使用上述方法将甲基碘盐原位转化为所需的结构2的化合物。

著录项

  • 公开/公告号IN225322B

    专利类型

  • 公开/公告日2008-11-28

    原文格式PDF

  • 申请/专利权人

    申请/专利号IN305/DEL/2003

  • 申请日2003-03-17

  • 分类号A61K31;

  • 国家 IN

  • 入库时间 2022-08-21 19:26:51

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