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【结 构 式】

【分子编号】58656

【品名】 

【CA登记号】

【 分 子 式 】C12H28NO3P

【 分 子 量 】265.333022

【元素组成】C 54.32% H 10.64% N 5.28% O 18.09% P 11.67%

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:(IV)

The reaction of colchicin (I) with aq. HCl at 100 C gives the monodemethylated compound (II), which is treated with H2O2 at 60 C to yield the dibenzocycloheptene derivative (III). The condensation of (III) with N,N-diethylphosphoramidic acid di-tert-butyl ester (IV) by means of tetrazole affords the phosphoric acid triester (V), which is finally treated with MCPBA to provide the target phosphoric acid monoester.

1 Blakey, D.C.; Davis, P.D.; Dougherty, G.J.; et al.; ZD6126: A novel vascular-targeting agent that causes selective destruction of tumor vasculature. Cancer Res 2002, 62, 24, 7247.
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) 18479 N-[(7S)-1,2,3,10-tetramethoxy-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide 64-86-8 C22H25NO6 详情 详情
(II) 58655 N-[(7S)-10-hydroxy-1,2,3-trimethoxy-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide C21H23NO6 详情 详情
(III) 47283 N-[(5S)-3-hydroxy-9,10,11-trimethoxy-6,7-dihydro-5H-dibenzo[a,c]cyclohepten-5-yl]acetamide C20H23NO5 详情 详情
(IV) 58656   C12H28NO3P 详情 详情
(V) 47285 (5S)-5-(acetamido)-9,10,11-trimethoxy-6,7-dihydro-5H-dibenzo[a,c]cyclohepten-3-yl di(tert-butyl) phosphate C28H40NO8P 详情 详情
Extended Information