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【结 构 式】

【分子编号】64261

【品名】3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)-1,3-dihydro-2H-indol-2-one

【CA登记号】

【 分 子 式 】C16H10ClF4NO2

【 分 子 量 】359.7072528

【元素组成】C 53.43% H 2.8% Cl 9.86% F 21.13% N 3.89% O 8.9%

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:(III)

The methylation of the phenolic OH of indanone (I) with tritium labeled methyl iodide and Cs2CO3 gives the methyl ether (II). The fluorination of the remaining OH of (II) with DAST yields the target compound as a racemic mixture, that is optically resolved by chiral HPLC.

1 Dischino, D.D.; Gribkoff, V.K.; Hewawasam, P.; Luke, G.M.; Rinehart, J.K.; Spears, T.L.; Starrett, J.E. Jr.; Synthesis of 3H and 14C labeled (S)-3-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-2H-indol-2-one, MaxiPost(TM). An agent for post-stroke neuroprotection. J Label Compd Radiopharm 2003, 46, 2, 139.
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) 64259 3-(5-chloro-2-hydroxyphenyl)-3-hydroxy-6-(trifluoromethyl)-1,3-dihydro-2H-indol-2-one C15H9ClF3NO3 详情 详情
(II) 39339 3-(5-chloro-2-methoxyphenyl)-3-hydroxy-6-(trifluoromethyl)-1,3-dihydro-2H-indol-2-one C16H11ClF3NO3 详情 详情
(II) 64260 3-(5-chloro-2-methoxyphenyl)-3-hydroxy-6-(trifluoromethyl)-1,3-dihydro-2H-indol-2-one C16H11ClF3NO3 详情 详情
(III) 43889 3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)-1,3-dihydro-2H-indol-2-one C16H10ClF4NO2 详情 详情
(III) 64261 3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)-1,3-dihydro-2H-indol-2-one C16H10ClF4NO2 详情 详情
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