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1H-Indole-2-carboxylic acid, 7-amino-, ethyl ester → N4-(3,5-dimethoxyphenyl)-N2-(2-ethoxycarbonylindol-7-yl)-5-fluoro-2,4-pyrimidinediamine

HRID 528266
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HRID 528266 반응식
Cl[C:2]1[N:7]=[C:6]([NH:8][C:9]2[CH:14]=[C:13]([O:15][CH3:16])[CH:12]=[C:11]([O:17][CH3:18])[CH:10]=2)[C:5]([F:19])=[CH:4][N:3]=1.[CH2:20]([O:22][C:23]([C:25]1[NH:26][C:27]2[C:32]([CH:33]=1)=[CH:31][CH:30]=[CH:29][C:28]=2[NH2:34])=[O:24])[CH3:21]>>[CH3:18][O:17][C:11]1[CH:10]=[C:9]([NH:8][C:6]2[C:5]([F:19])=[CH:4][N:3]=[C:2]([NH:34][C:28]3[CH:29]=[CH:30][CH:31]=[C:32]4[C:27]=3[NH:26][C:25]([C:23]([O:22][CH2:20][CH3:21])=[O:24])=[CH:33]4)[N:7]=2)[CH:14]=[C:13]([O:15][CH3:16])[CH:12]=1
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참가 물질

3

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HCID 111381941H-Indole-2-carboxylic acid, 7-amino-, ethyl esterHCID 220606942-chloro-N4-(3,5-dimethoxyphenyl)-5-fluoro-4-pyrimidineamine

생성물 1

HCID 22060274N4-(3,5-dimethoxyphenyl)-N2-(2-ethoxycarbonylindol-7-yl)-5-fluoro-2,4-pyrimidinediamine

실험 절차

In like manner to the preparation of N4-(3,4-ethylenedioxyphenyl)-5-fluoro-N2-(3-hydroxyphenyl)-2,4-pyrimidinediamine, the reaction of 2-chloro-N4-(3,5-dimethoxyphenyl)-5-fluoro-4-pyrimidineamine with 2-ethoxycarbonyl-7-aminoindole gave N4-(3,5-dimethoxyphenyl)-N2-(2-ethoxycarbonylindol-7-yl)-5-fluoro-2,4-pyrimidinediamine. LCMS: ret. time: 24.21 min.; purity: 91%; MS (m/e): 452 (MH+).

후처리

  1. customIn like manner to the preparation of N4-(3,4-ethylenedioxyphenyl)-5-fluoro-N2-(3-hydroxyphenyl)-2,4-pyrimidinediamine

출처 및 근거

ORD 기록
ord-9fe2056d7852449c83941cfab8ad18bb
출처 데이터셋
uspto-grants-2016_05
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US09346765B2

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