1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine) → (5-Bromo-imidazo[1,2-a]pyrazin-8-yl)-[4-(4-pyridin-2-yl-[1,2,3]triazol-1-yl)-phenyl]amine

HRID 1366151

반응식

HRID 1366151 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.[N:44]1[CH:49]=[CH:48][CH:47]=[CH:46][C:45]=1[C:50]1[N:51]=[N:52][N:53]([C:55]2[CH:60]=[CH:59][C:58]([NH2:61])=[CH:57][CH:56]=2)[CH:54]=1.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:61][C:58]2[CH:59]=[CH:60][C:55]([N:53]3[CH:54]=[C:50]([C:45]4[CH:46]=[CH:47][CH:48]=[CH:49][N:44]=4)[N:51]=[N:52]3)=[CH:56][CH:57]=2)=[N:36][CH:35]=1

참가 물질

8

실험 절차

In the same way as described for Compound 90, step 1, using 5,8-dibromoimidazo[1,2-a]pyrazine (80.5 mg, 0.291 mmol), 4-(4-pyridin-2-yl-[1,2,3]triazol-1-yl)-phenylamine (68.3 g, 0.288 mmol), NaOtBu (38.2 mg, 0.403 mmol), Pd2(dba)3 (10.5 mg, 0.0115 mmol), Xantphos (13.3 mg, 0.023mmol) and toluene (4 mL). The crude material is purified by silica gel column chromatography eluting with 98:2 DCM:MeOH followed by 97:3 DCM:MeOH affording the title compound (52.8 mg, 42%).

후처리

  1. customThe crude material is purified by silica gel column chromatography
  2. washeluting with 98:2 DCM

출처 및 근거

ORD 기록
ord-cf5af2bf34b34aa8992337fb51c4d67b
출처 데이터셋
uspto-grants-2011_02
특허 번호
US07893058B2

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