N'-(3-Cyano-pyridin-2-yl)-N,N-dimethyl-formamidine → N-(4-Bromo-benzyl)-4-(4-hydroxy-phenylsulfanyl)-3-(pyrido[2,3-d]pyrimidin-4-ylamino)-benzamide
反応式
[NH2:1][C:2]1[CH:3]=[C:4]([CH:16]=[CH:17][C:18]=1[S:19][C:20]1[CH:25]=[CH:24][C:23]([OH:26])=[CH:22][CH:21]=1)[C:5]([NH:7][CH2:8][C:9]1[CH:14]=[CH:13][C:12]([Br:15])=[CH:11][CH:10]=1)=[O:6].C([C:29]1[C:30]([N:35]=[CH:36][N:37]([CH3:39])C)=[N:31][CH:32]=[CH:33][CH:34]=1)#N.NC1C=C(C=CC=1SC1C=CC(O)=CC=1)C(NC1C=CC(Br)=CC=1)=O>>[Br:15][C:12]1[CH:13]=[CH:14][C:9]([CH2:8][NH:7][C:5](=[O:6])[C:4]2[CH:16]=[CH:17][C:18]([S:19][C:20]3[CH:25]=[CH:24][C:23]([OH:26])=[CH:22][CH:21]=3)=[C:2]([NH:1][C:39]3[C:29]4[CH:34]=[CH:33][CH:32]=[N:31][C:30]=4[N:35]=[CH:36][N:37]=3)[CH:3]=2)=[CH:10][CH:11]=1参加物
4
反応物 3
生成物 1
実験手順
The product of Example 33A was reacted with the product of Example 29A using the procedure of Example 22C substituting the product of Example 33A for the product of Example 22B and substituting the product of Example 29A for the product of Example 8E to provide the crude title compound which was purified by column chromatography on silica gel using methanol/dichloromethane as eluent to provide the title product (26 mg, 26%). 1H NMR (300 MHz, DMSO-D6) δ ppm: 4.41 (d, J=5.88 Hz, 2 H) 6.76-6.96 (m, 1 H) 6.83 (d, J=8.46 Hz, 2 H) 7.20-7.33 (m, 4 H) 7.51 (d, J=8.46 Hz, 2 H) 7.58-7.80 (m, 2 H) 7.82-7.97 (m, 1 H) 8.52-8.69 (m, 1 H) 8.86-9.18 (m, 3 H) 9.94 (s, 1 H) 10.28 (s, 1 H); MS (ESI+) m/z 558/560 (M+H)+.
後処理
- customto provide the crude title compound which
- customwas purified by column chromatography on silica gel
出典と根拠
- ORDレコード
- ord-26fe5a83dacd4a8b823f07e551fa2485
- 出典データセット
- uspto-grants-2011_03
- 特許番号
- US07910595B2
反応ノート
読み込み中…