【药物名称】TAX-109, 109881, XRP-9881, RPR-109881A
化学结构式(Chemical Structure):
参考文献No.22186
标题:7,8-Cyclopropataxones
作者:Chen, S.-H.; Farina, V. (Bristol-Myers Squibb Co.)
来源:CA 2099211; EP 0577083; JP 1994179665; JP 1994179666; JP 2001199974; US 5254580
合成路线图解说明:

The reaction of taxol (I) with benzyloxycarbonyl chloride and DIEA in dichloromethane gives the protected compound (II), which is treated with DAST in the same solvent to yield the cyclopropa taxol (III). The hydrogenolysis of (III) with H2 over Pd/C affords compound (IV), which is deacylated with tetrabutylammonium borohydride in dichloromethane to provide the cyclopropa baccatin (V). The acylation of (V) with azetidinone (VI) by means of BuLi in THF gives the silylated taxoid (VII), which is finally desilylated with HCl in acetonitrile to afford the target compound.

参考文献No.24134
标题:Novel taxoids, preparation thereof and pharmaceutical compsns. containing same
作者:Bouchard, H.; Buourzat, J.-D.; Commer鏾n, A. (Aventis Pharma SA)
来源:EP 0673372; FR 2698871; JP 1996504425; JP 1998291930; US 5814658; WO 9413654
合成路线图解说明:

The reaction of the taxane derivative (I) with trifluoromethanesulfonic anhydride gives the monotriflate (II), which is treated with sodium azide in hot acetonitrile to yield the cyclopropa derivative (III). The cleavage of the oxazolidine ring of (III) by means of formic acid affords the 3-amino-2-hydroxy derivative (IV), which is finally acylated with tert-butoxycarbonyl anhydride to provide the target taxoid derivative.

参考文献No.47570
标题:Method for treating abnormal cell proliferation in the brain
作者:Renard, A.; Bissery, M.-C. (Aventis Pharma SA)
来源:US 6156789
合成路线图解说明:

The reaction of the taxane derivative (I) with trifluoromethanesulfonic anhydride gives the monotriflate (II), which is treated with sodium azide in hot acetonitrile to yield the cyclopropa derivative (III). The cleavage of the oxazolidine ring of (III) by means of formic acid affords the 3-amino-2-hydroxy derivative (IV), which is finally acylated with tert-butoxycarbonyl anhydride to provide the target taxoid derivative.

参考文献No.49598
标题:7-Halo and 7beta,8beta-methano-taxols, antineoplastic use and pharmaceutical compsns. containing them
作者:Skulnick, H.I.; Johnson, R.A.; Midy, E.G.; Kelly, R.C.; Hester, J.B. Jr. (Pharmacia Corp.)
来源:EP 0674630; WO 9413655
合成路线图解说明:

The reaction of the taxoid compound (I) with DAST gives the cyclopropataxoid compound (II), which is finally deprotected with Zn and HOAc to yield the target compound.

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