Patent ID: 6080735
Filing Date: 2000-06-27
Classification: A61P,C07J

Abstract:
A process for preparing estra-1,3,5(10)-trien compounds selected from the group consisting of:17.beta.-hydroxy-14.alpha.,15.alpha.-methylene-estra-1,3,5(10)-trien-3-yl N,N-dimethyl-sulfamate,17.beta.-hydroxy-14.alpha.,15.alpha.-methylene-estra-1,3,5(10)-trien-3-yl N-methyl-sulfamate,17.beta.-hydroxy-14.alpha.,15.alpha.-methylene-estra-1,3,5(10)-trien-3-yl sulfa-mate,17.beta.-hydroxy-14.alpha.,15.alpha.-methylene-estra-1,3,5(10),7-tetraene-3 -yl N,N-dimethylsulfamate,17.beta.-hydroxy-14.alpha.,15.alpha.-methylene-estra-1,3,5(10),8-tetraene-3 -yl N,N-dimethylsulfamate,17.beta.-hydroxy-14.alpha.,17.alpha.-vinylene-estra-1,3,5(10)-trien-3-yl N,N-dimethylsulfamate,17.beta.-hydroxy-11.beta.-methoxy-19-nor-17.alpha.-pregn-1,3,5(10)-trien-20 -in-3-yl N,N-dimethylsulfamate,11.beta.-methoxy-17-oxo-estra-1,3,5(10)-trien-3-yl sulfamate,17.beta.-hydroxy-estra-1,3,5(10)-trien-3-yl N-methylsulfamate,17.beta.-hydroxy-estra-1,3,5(10)-trien-3-yl sulfamate,17.beta.-hydroxy-estra-1,3,5(10), 6,8-pentaene-3-yl sulfamate,17.beta.-hydroxy-estra-1,3,5(10)-trien-3-yl sulfamate,1.alpha. . 17.beta.-dihydroxy-estra-1,3,5(10)-trien-3-yl N,N-dimethyl-sulfamate,16.alpha.,17.beta.-dihydroxy-estra-1,3,5(10)-trien-3-yl N-methysulfamate,16.alpha.,17.beta.-dihydroxy-estra-1,3,5(10)-trien-3-yl sulfamate,17.beta.-hydroxy-14.alpha.,17.alpha.-vinylene-estra-1,3,5(10)-trien-3-yl sulfamate,14.alpha.,17.alpha.-ethylene-17.beta.-hydroxy-estra-1,3,5(10)-trien-3-yl N-methyl-sulfamate,16.alpha.,17.alpha.-dihydroxy14.alpha., 17.alpha.-ethylene-estra-1,3,5(10)-trien-3-yl sulfamate, and17.beta.-hydroxy-11.beta.-methoxy-19-nor-17.alpha.-pregn-1,3,5(10)-trien-20 -in-3-yl sulfamate,wherein said process comprises reacting an estra-1,3,5(1 0)-trien-3-ol in a manner known per se with an appropriately substituted amidosulphonyl chloride to obtain the esterification of the 3-OH group of estra-1,3,5(10)-trien compounds.