반응식
Br[C:2]1[CH:3]=[C:4]([C:9]2[NH:10][C:11]3[C:12]([N:17]=2)=[N:13][CH:14]=[CH:15][CH:16]=3)[C:5]([NH2:8])=[N:6][CH:7]=1.[CH3:18][N:19]1[CH:23]=[C:22](B2OC(C)(C)C(C)(C)O2)[CH:21]=[N:20]1.C(=O)([O-])[O-].[Na+].[Na+]>CN(C)C=O.C1C=CC([P]([Pd]([P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)([P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)[P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)=CC=1>[NH:10]1[C:11]2[C:12](=[N:13][CH:14]=[CH:15][CH:16]=2)[N:17]=[C:9]1[C:4]1[C:5]([NH2:8])=[N:6][CH:7]=[C:2]([C:22]2[CH:21]=[N:20][N:19]([CH3:18])[CH:23]=2)[CH:3]=1참가 물질
6
반응물 3
생성물 1
시약·촉매·용매 2
실험 절차
58 mg (0.200 mmol) of 5-bromo-3-(1H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-ylamine and 45.8 mg (0.220 mmol) of 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole are suspended in 2 ml of N,N-dimethylformamide in a nitrogen-filled microwave vessel, and 0.57 ml (1.142 mmol) of 2M sodium carbonate solution and 23.1 mg (0.020 mmol) of tetrakis(triphenylphosphine)palladium(0) are added. The reaction solution is irradiated with microwaves for 30 min at 120° C. in the Biotage SmithSynthesizer. The reaction mixture is evaporated to dryness, and the residue is purified by means of RP-HPLC, giving 3-(1H-imidazo[4,5-b]pyridin-2-yl)-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-ylamine; HPLC-MS [M+H]+ 292.2;
후처리
- additionfilled microwave vessel
- customThe reaction solution is irradiated with microwaves for 30 min at 120° C. in the Biotage SmithSynthesizer
- customThe reaction mixture is evaporated to dryness
- customthe residue is purified by means of RP-HPLC
출처 및 근거
- ORD 기록
- ord-a1ef29d4a7fb4ec281e9f0fd034bb37c
- 출처 데이터셋
- uspto-grants-2014_02
- 특허 번호
- US08648201B2
연결된 노트
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