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【结 构 式】

【分子编号】49338

【品名】5-[(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-bis(acetoxy)-2-(benzoyloxy)-1,9-dihydroxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0(3,10).0(4,7)]heptadec-13-en-15-yl] 3-(tert-butyl) (4S,5R)-2,2-dimethyl-4-phenyl-1,3-oxazolidine-3,5-dicarboxylate

【CA登记号】

【 分 子 式 】C48H59NO15

【 分 子 量 】889.9942

【元素组成】C 64.78% H 6.68% N 1.57% O 26.97%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(I)

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.

1 Bouchard, H.; Buourzat, J.-D.; Commercon, A. (Aventis Pharma SA); Novel taxoids, preparation thereof and pharmaceutical compsns. containing same. EP 0673372; FR 2698871; JP 1996504425; JP 1998291930; US 5814658; WO 9413654 .
2 Renard, A.; Bissery, M.-C. (Aventis Pharma SA); Method for treating abnormal cell proliferation in the brain. US 6156789 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 49338 5-[(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-bis(acetoxy)-2-(benzoyloxy)-1,9-dihydroxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0(3,10).0(4,7)]heptadec-13-en-15-yl] 3-(tert-butyl) (4S,5R)-2,2-dimethyl-4-phenyl-1,3-oxazolidine-3,5-dicarboxylate C48H59NO15 详情 详情
(II) 49339 5-((1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-bis(acetoxy)-2-(benzoyloxy)-1-hydroxy-10,14,17,17-tetramethyl-11-oxo-9-[[(trifluoromethyl)sulfonyl]oxy]-6-oxatetracyclo[11.3.1.0(3,10).0(4,7)]heptadec-13-en-15-yl) 3-(tert-butyl) (4S,5R)-2,2-dimethyl-4-phenyl-1,3-oxazolidine-3,5-dicarboxylate C49H58F3NO17S 详情 详情
(III) 49340 5-[(1S,2S,3R,4S,7R,9S,11R,13R,16S)-4,13-bis(acetoxy)-2-(benzoyloxy)-1-hydroxy-15,18,18-trimethyl-12-oxo-6-oxapentacyclo[12.3.1.0(3,11).0(4,7).0(9,11)]octadec-14-en-16-yl] 3-(tert-butyl) (4S,5R)-2,2-dimethyl-4-phenyl-1,3-oxazolidine-3,5-dicarboxylate C48H57NO14 详情 详情
(IV) 39341 methyl 2-(5-chloro-2-methoxyphenyl)acetate C10H11ClO3 详情 详情
Extended Information