반응식
Cl[C:2]1[CH:7]=[CH:6][C:5]([CH2:8][C@@H:9]([C:13]2[CH:18]=[CH:17][CH:16]=[C:15]([C:19]#[N:20])[CH:14]=2)[C@@H:10]([NH2:12])[CH3:11])=[CH:4][CH:3]=1.[CH3:21][C:22]([O:27][C:28]1[CH:33]=[C:32]([C:34]([F:37])([F:36])[F:35])[CH:31]=[CH:30][N:29]=1)([CH3:26])[C:23]([OH:25])=O.CN1CC[O:42][CH2:41]C1>C(Cl)Cl>[C:19]([C:15]1[CH:14]=[C:13]([C@H:9]([CH2:8][C:5]2[CH:6]=[CH:7][C:2]([O:42][CH3:41])=[CH:3][CH:4]=2)[C@@H:10]([NH:12][C:23](=[O:25])[C:22]([O:27][C:28]2[CH:33]=[C:32]([C:34]([F:37])([F:36])[F:35])[CH:31]=[CH:30][N:29]=2)([CH3:21])[CH3:26])[CH3:11])[CH:18]=[CH:17][CH:16]=1)#[N:20]참가 물질
반응물 3
생성물 1
시약·촉매·용매 1
실험 절차
To a solution of N-(1S, 2S)-[3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]amine (Reference Example 4, 0.60 g, 2.1 mol) and 2-(4-trifluoromethyl-2-pyridyloxy)-2-methylpropionic acid (Reference Example 13, 0.58 g, 2.4 mmol) in 10 mL of CH2Cl2 was added N-methylmorpholine (0.46 mL, 4.2 mmol) and tris(pyrrolindinyl)phosphonium hexafluorophosphate (1.6 g, 3.2 mmol). After stirring at room temperature overnight, the reaction mixture was loaded onto a silica gel column eluted with 30% EtOAc in hexane to give the title compound. 1H NMR (500 MHz, CD3OD): δ 8.19 (d, 1H), 7.48 (d, 1H), 7.38-7.35 (m, 2H), 7.31 (d, 1H), 7.18 (s, 1H), 7.11 (d, 1H), 7.03 (d, 2H), 6.67 (d, 2H), 4.23 (m, 1H), 3.01 (dd, 1H), 2.83 (m, 1H), 2.61 (dd, 1H), 1.76 (s, 3H), 1.72 (s, 3H), 0.79 (d, 3H).
후처리
- washeluted with 30% EtOAc in hexane
출처 및 근거
- ORD 기록
- ord-38e08ebd253649279bd3959214c4b68e
- 출처 데이터셋
- uspto-grants-2010_07
- 특허 번호
- US07754188B2
연결된 노트
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