반응식
OC1C=CC(CNC(=O)C2C=CC(NC3C4N(C=CN=4)C(C4C=NNC=4)=CN=3)=CC=2)=CC=1.[Br:33][C:34]1[N:39]2[CH:40]=[CH:41][N:42]=[C:38]2[C:37](Br)=[N:36][CH:35]=1.[CH3:44][N:45]([CH2:47][C:48]1[N:49]=[N:50][N:51]([C:53]2[CH:58]=[CH:57][C:56]([NH2:59])=[CH:55][CH:54]=2)[CH:52]=1)[CH3:46].CC([O-])(C)C.[Na+].CC1(C)C2C(=C(P(C3C=CC=CC=3)C3C=CC=CC=3)C=CC=2)OC2C(P(C3C=CC=CC=3)C3C=CC=CC=3)=CC=CC1=2>C1C=CC(/C=C/C(/C=C/C2C=CC=CC=2)=O)=CC=1.C1C=CC(/C=C/C(/C=C/C2C=CC=CC=2)=O)=CC=1.C1C=CC(/C=C/C(/C=C/C2C=CC=CC=2)=O)=CC=1.[Pd].[Pd].C1(C)C=CC=CC=1>[Br:33][C:34]1[N:39]2[CH:40]=[CH:41][N:42]=[C:38]2[C:37]([NH:59][C:56]2[CH:55]=[CH:54][C:53]([N:51]3[CH:52]=[C:48]([CH2:47][N:45]([CH3:46])[CH3:44])[N:49]=[N:50]3)=[CH:58][CH:57]=2)=[N:36][CH:35]=1참가 물질
8
반응물 5
HCID 6360441,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)
HCID 23676156Sodium t-butoxide
HCID 24857547N-(4-Hydroxybenzyl)-4-[5-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-ylamino]benzamide
HCID 534859495,8-Dibromoimidazo[1,2-a]pyrazine
HCID 590230944-(4-Dimethylaminomethyl-[1,2,3]triazol-1-yl)-phenylamine생성물 1
시약·촉매·용매 2
실험 절차
In the same way as described for Compound 90, step 1, using 5,8-dibromoimidazo[1,2-a]pyrazine (116.9 mg, 0.422 mmol), 4-(4-dimethylaminomethyl-[1,2,3]triazol-1-yl)-phenylamine (91.7 g, 0.422 mmol), NaOtBu (56.8 mg, 0.591 mmol), Pd2(dba)3 (15.5 mg, 0.0169 mmol), Xantphos (19.5 mg, 0.0337 mmol) and toluene (5 mL). The crude product is purified by Isolute FlashSilicaII cartridge chromatography eluting with 99:1 DCM/NH3 (7M in MeOH), followed by 97:3 DCM:NH3 (7M in MeOH). The title compound (63 mg, 36%) is isolated after a second column chromatography purification eluting with 97:3 DCM:NH3 (7M in MeOH).
후처리
- customThe crude product is purified by Isolute FlashSilicaII cartridge chromatography
- washeluting with 99:1 DCM/NH3 (7M in MeOH)
출처 및 근거
- ORD 기록
- ord-b933f04f976e4947aeff683e4abe8972
- 출처 데이터셋
- uspto-grants-2012_05
- 특허 번호
- US08173656B2
연결된 노트
불러오는 중…