-药物合成数据库

【药物名称】

化学结构式(Chemical Structure):

参考文献No.	42199
标题:	Estra-1,3,5(10)-triene-7alpha-thioethers
作者:	Jirkovsky, I.; Miller, C.P.; Tran, B.D. (American Home Products Corp.)
来源:	EP 1025116; WO 9920646

合成路线图解说明: Displacement of the 7-alpha bromo substituent of bromoketone (I) by N-butyl-N-methyl-11-mercaptoundecamide (II) with retention of configuration provided the 7-alpha thioether (III). The keto group of (III) was reduced with NaBH4 to alcohol (IV), which was further deoxygenated to (V) by means of triethylsilane and trifluoroacetic acid. Finally, basic hydrolysis of the acetate esters of (V) furnished the title compound.

参考文献No.	565105
标题:	Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives
作者:	Miller, C.P.; Jirkovsku, I.; Tran, B.D.; Harris, H.A.; Moran, R.A.; Komm, B.S.
来源:	Bioorg Med Chem Lett 2000,10(2),147

合成路线图解说明: Displacement of the 7-alpha bromo substituent of bromoketone (I) by N-butyl-N-methyl-11-mercaptoundecamide (II) with retention of configuration provided the 7-alpha thioether (III). The keto group of (III) was reduced with NaBH4 to alcohol (IV), which was further deoxygenated to (V) by means of triethylsilane and trifluoroacetic acid. Finally, basic hydrolysis of the acetate esters of (V) furnished the title compound.