Potassium Carbonate → 5-(5-chloro-2-thienyl)-3-(1-{[3-(1-pyrrolidinyl)propyl]sulfonyl}-4-piperidinyl)-1H-indole-7-carboxamide
반응식
N1([CH2:6][CH2:7][S:8]([N:11]2[CH2:16][CH2:15][CH:14]([C:17]3[C:25]4[C:20](=[C:21]([C:31]([NH2:33])=[O:32])[CH:22]=[C:23](C5C=CSC=5)[CH:24]=4)[NH:19][CH:18]=3)[CH2:13][CH2:12]2)(=[O:10])=[O:9])CCCC1.[Cl:34][C:35]1[S:39][C:38](B(O)O)=[CH:37][CH:36]=1.C(=O)([O-])[O-].[K+].[K+].O1[CH2:54][CH2:53]OCC1>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>[Cl:34][C:35]1[S:39][C:38]([C:23]2[CH:24]=[C:25]3[C:20](=[C:21]([C:31]([NH2:33])=[O:32])[CH:22]=2)[NH:19][CH:18]=[C:17]3[CH:14]2[CH2:13][CH2:12][N:11]([S:8]([CH2:7][CH2:6][CH2:16][N:11]3[CH2:54][CH2:53][CH2:13][CH2:12]3)(=[O:10])=[O:9])[CH2:16][CH2:15]2)=[CH:37][CH:36]=1참가 물질
7
반응물 4
생성물 1
시약·촉매·용매 2
실험 절차
The title compound was prepared following the general procedure described in intermediate 16. Thus, 15-bromo-3-(1-{[3-(1-pyrrolidinyl)propyl]sulfonyl}-4-piperidinyl)-1H-indole-7-carboxamide (95 mg, 0.19 mmol) in dioxane (3 mL) and water (1 mL), 5-chloro-2-thienylboronic acid (123 mg, 0.76 mmol), Pd(PPh3)4 (22.2 mg, 10%) and potassium carbonate (211 mg, 1.52 mmol) in dioxane (3.0 mL) and water (1.0 mL) were reacted to form the desired product which was purified by reverse phase HPLC eluting with 10% B to 80% B, where A=H2O (0.1% trifluoroacetic acid) and B=CH3CN (0.1% trifluoroacetic acid) to give the title compound (11 mg, 11%).
후처리
- customThe title compound was prepared
출처 및 근거
- ORD 기록
- ord-8d29cd79ba3c4f86a1efb03bb449f4bd
- 출처 데이터셋
- uspto-grants-2010_12
- 특허 번호
- US07858796B2
반응 노트
불러오는 중…