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【结 构 式】

【分子编号】34381

【品名】9H-fluoren-9-ylmethyl 2-chloro-4-[((3S,10R,16S)-3-isobutyl-6,6-dimethyl-2,5,9,12-tetraoxo-16-[(1R)-1-[(2R,3S)-3-phenyloxiranyl]ethyl]-1,4-dioxa-8,11-diaza-13-cyclohexadecen-10-yl)methyl]phenylcarbamate

【CA登记号】

【 分 子 式 】C50H54ClN3O9

【 分 子 量 】876.44628

【元素组成】C 68.52% H 6.21% Cl 4.05% N 4.79% O 16.43%

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:(XV)

Further epoxidation of (XIV) with m-CPBA led to a mixture of alpha and beta diastereomeric epoxides, which were separated by RP-HPLC to afford the major beta-epoxide (XV). Deprotection of (XV) with piperidine gave aniline (XVI). This was finally alkylated using iodomethane in the presence of K2CO3 to produce the title dimethylamine.

1 Schultz, R.M.; Andis, S.L.; Ray, J. E.; Patel, V.F.; Kennedy, J.H.; Novel cryptophycin antitumor agents: Synthesis and cytotoxicity of fragment "B" analogues. J Med Chem 1999, 42, 14, 2588.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(XIV) 34380 9H-fluoren-9-ylmethyl 2-chloro-4-([(3S,10R,16S)-3-isobutyl-6,6-dimethyl-16-[(1R,2E)-1-methyl-3-phenyl-2-propenyl]-2,5,9,12-tetraoxo-1,4-dioxa-8,11-diaza-13-cyclohexadecen-10-yl]methyl)phenylcarbamate C50H54ClN3O8 详情 详情
(XV) 34381 9H-fluoren-9-ylmethyl 2-chloro-4-[((3S,10R,16S)-3-isobutyl-6,6-dimethyl-2,5,9,12-tetraoxo-16-[(1R)-1-[(2R,3S)-3-phenyloxiranyl]ethyl]-1,4-dioxa-8,11-diaza-13-cyclohexadecen-10-yl)methyl]phenylcarbamate C50H54ClN3O9 详情 详情
(XVI) 34382 (3S,10R,16S)-10-(4-amino-3-chlorobenzyl)-3-isobutyl-6,6-dimethyl-16-[(1R)-1-[(2R,3S)-3-phenyloxiranyl]ethyl]-1,4-dioxa-8,11-diaza-13-cyclohexadecene-2,5,9,12-tetrone C35H44ClN3O7 详情 详情
Extended Information