【药物名称】SCH-60663
化学结构式(Chemical Structure):
参考文献No.33304
标题:Sugar-substd. 2-azetidinones useful as hypocholesterolemic agents
作者:Yumibe, N.P.; Alton, K.B.; Van Heek, M.; Davis, H.R.; Vaccaro, W.D. (Schering Corp.)
来源:EP 0877750; JP 1998512592; WO 9716455
合成路线图解说明:

Protected glucuronic acid (I) was converted to trichloroacetimidate (II) by treatment with trichloroacetonitrile and Cs2CO3.

合成路线图解说明:

Diol (III) was acetylated with Ac2O in the presence of dimethylaminopyridine to yield diester (IV), which was selectively hydrolyzed to monoacetate (V) by means of methanolic guanidine. Coupling of phenol (V) with imidate (II) by means of boron trifluoride etherate furnished the protected glucuronide (VI). The ester groups of (VI) were finally hydrolyzed by treatment with triethylamine in aqueous methanol.

参考文献No.43620
标题:Sugar-substd. 2-azetidinones useful as hypocholesterolemic agents
作者:Yumibe, N.P.; Alton, K.B.; Vaccaro, W.D.; Davis, H.R.; Van Heek, M. (Schering Corp.)
来源:US 5756470
合成路线图解说明:

Protected glucuronic acid (I) was converted to trichloroacetimidate (II) by treatment with trichloroacetonitrile and Cs2CO3.

合成路线图解说明:

Diol (III) was acetylated with Ac2O in the presence of dimethylaminopyridine to yield diester (IV), which was selectively hydrolyzed to monoacetate (V) by means of methanolic guanidine. Coupling of phenol (V) with imidate (II) by means of boron trifluoride etherate furnished the protected glucuronide (VI). The ester groups of (VI) were finally hydrolyzed by treatment with triethylamine in aqueous methanol.

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