반응식
[NH2:1][C@H:2]1[CH2:6][CH2:5][CH2:4][C@H:3]1[NH:7][C:8]1[N:17]=[CH:16][C:15]2[C:10](=[CH:11][CH:12]=[C:13]([C:18]3[CH:29]=[CH:28][C:21]([C:22]([NH:24][CH:25]4[CH2:27][CH2:26]4)=[O:23])=[CH:20][C:19]=3[O:30][CH3:31])[CH:14]=2)[N:9]=1.[C:32](O)(=[O:35])[C:33]#[CH:34].CN(C(ON1N=NC2C=CC=NC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F.CCN(C(C)C)C(C)C>ClCCl>[CH:25]1([NH:24][C:22](=[O:23])[C:21]2[CH:28]=[CH:29][C:18]([C:13]3[CH:14]=[C:15]4[C:10](=[CH:11][CH:12]=3)[N:9]=[C:8]([NH:7][C@@H:3]3[CH2:4][CH2:5][CH2:6][C@@H:2]3[NH:1][C:32](=[O:35])[C:33]#[CH:34])[N:17]=[CH:16]4)=[C:19]([O:30][CH3:31])[CH:20]=2)[CH2:27][CH2:26]1참가 물질
6
반응물 4
생성물 1
시약·촉매·용매 1
실험 절차
A mixture of 4-(2-(((1R,2S)-2-aminocyclopentyl)amino)quinazolin-6-yl)-N-cyclopropyl-3-methoxybenzamide (0.11 mmol), propiolic acid (0.010 mL, 0.17 mmol), HATU (64 mg, 0.17 mmol) and DIEA (0.06 mL, 0.34 mmol) in dichloromethane (1.5 mL) was stirred at room temperature for 45 minutes. LC-MS indicated complete consumption of SM. The reaction mixture was purified by silica gel chromatography to yield N-cyclopropyl-3-methoxy-4-(2-(((1R,2S)-2-propiolamidocyclopentyl)amino)quinazolin-6-yl)benzamide (Compound 13) (35 mg, 69%). MS (ES+) C27H27N5O3 requires: 469, found: 470 [M+H]+.
후처리
- customconsumption of SM
- customThe reaction mixture was purified by silica gel chromatography
출처 및 근거
- ORD 기록
- ord-9184703973c84936a1b917438babccd9
- 출처 데이터셋
- uspto-grants-2016_09
- 특허 번호
- US09434700B2
연결된 노트
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