1-(3-Fluorobenzyl)-1H-pyrazole-4-carboxylic acid → HCID 58117360、化合物

反応式

[C:1]([O:5][C:6]([N:8]1[C:16]2[C:11](=[CH:12][CH:13]=[CH:14][CH:15]=2)[CH:10]=[C:9]1[C:17]1[C:18](=[O:33])[N:19]([CH2:25][O:26][CH2:27][CH2:28][Si:29]([CH3:32])([CH3:31])[CH3:30])[C:20]([CH3:24])=[C:21]([NH2:23])[CH:22]=1)=[O:7])([CH3:4])([CH3:3])[CH3:2].[F:34][C:35]1[CH:36]=[C:37]([CH:47]=[CH:48][CH:49]=1)[CH2:38][N:39]1[CH:43]=[C:42]([C:44](O)=[O:45])[CH:41]=[N:40]1.FC1C=CC(CN2C=C(C(O)=O)C=N2)=CC=1>>[C:1]([O:5][C:6]([N:8]1[C:16]2[C:11](=[CH:12][CH:13]=[CH:14][CH:15]=2)[CH:10]=[C:9]1[C:17]1[C:18](=[O:33])[N:19]([CH2:25][O:26][CH2:27][CH2:28][Si:29]([CH3:30])([CH3:32])[CH3:31])[C:20]([CH3:24])=[C:21]([NH:23][C:44]([C:42]2[CH:41]=[N:40][N:39]([CH2:38][C:37]3[CH:47]=[CH:48][CH:49]=[C:35]([F:34])[CH:36]=3)[CH:43]=2)=[O:45])[CH:22]=1)=[O:7])([CH3:4])([CH3:3])[CH3:2]

参加物

反応物 3

HCID 116657161-(3-Fluorobenzyl)-1H-pyrazole-4-carboxylic acid

HCID 43565332HCID 43565332、化合物

HCID 58117460HCID 58117460、化合物2 回

生成物 1

HCID 58117360HCID 58117360、化合物

実験手順

The title compound was prepared according to the experimental used in Example 20, Step 4 with intermediate (7d), 2-[5-amino-6-methyl-2-oxo-1-(2-trimethylsilanyl-ethoxymethyl)-1,2-dihydropyridin-3-yl]indole-1-carboxylic acid tert-butyl ester, and 1-(3-Fluoro-benzyl)-1H-pyrazole-4-carboxylic acid, which was synthesised according to the protocol described for intermediate (6e) in Example 21. The resultant crude product was purified by flash chromatography on SiO2 with hexane—50% ethyl acetate/hexane (gradient) to afford the title compound as a yellow oil, 80 mg, 70%.