반응식
Cl[C:2]1[N:7]=[C:6]([N:8]2[CH2:13][CH2:12][O:11][CH2:10][CH2:9]2)[N:5]=[C:4]([NH:14][C:15]2[S:16][CH:17]=[C:18]([C:20]3[CH:25]=[CH:24][CH:23]=[CH:22][CH:21]=3)[N:19]=2)[CH:3]=1.CC1(C)C(C)(C)OB([C:34]2[C:35]([C:41]([F:44])([F:43])[F:42])=[CH:36][C:37]([NH2:40])=[N:38][CH:39]=2)O1>O1CCOCC1.C(=O)([O-])[O-].[Na+].[Na+].[Pd](Cl)Cl.C1(P(C2C=CC=CC=2)[C-]2C=CC=C2)C=CC=CC=1.[C-]1(P(C2C=CC=CC=2)C2C=CC=CC=2)C=CC=C1.[Fe+2]>[NH2:40][C:37]1[N:38]=[CH:39][C:34]([C:2]2[N:7]=[C:6]([N:8]3[CH2:13][CH2:12][O:11][CH2:10][CH2:9]3)[N:5]=[C:4]([NH:14][C:15]3[S:16][CH:17]=[C:18]([C:20]4[CH:25]=[CH:24][CH:23]=[CH:22][CH:21]=4)[N:19]=3)[CH:3]=2)=[C:35]([C:41]([F:44])([F:42])[F:43])[CH:36]=1참가 물질
6
반응물 2
생성물 1
시약·촉매·용매 3
실험 절차
A solution of N-(6-chloro-2-morpholinopyrimidin-4-yl)-4-phenylthiazol-2-amine (15 mg, 0.040 mmol), 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-4-(trifluoromethyl)pyridin-2-amine (23 mg, 0.080 mmol) and 1,1′-bis(diphenylphosphino)ferrocene palladium (II) chloride (6.6 mg, 0.0080 mmol) in 0.5 mL of 1,4-dioxane and 0.05 mL of 2 M aq. sodium carbonate was heated in the microwave at 120° C. for 600 seconds. The crude product was purified by reverse phase prep HPLC to give N-(6-(6-amino-4-(trifluoromethyl)pyridin-3-yl)-2-morpholinopyrimidin-4-yl)-4-phenylthiazol-2-amine. LC/MS (m/z): 500 (MH+), Rt 2.46 minutes.
후처리
- customThe crude product was purified by reverse phase prep HPLC
출처 및 근거
- ORD 기록
- ord-9aca640de49a4df3816e36a096f8d937
- 출처 데이터셋
- uspto-grants-2012_07
- 특허 번호
- US08217035B2
연결된 노트
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