2,5-Dichlorobenzenesulfonyl chloride → HCID 57732809, 화합물

HRID 562295노트

반응식

HRID 562295 반응식
[NH2:1][CH2:2][C:3]1[CH:4]=[C:5]([C:9]2[CH:10]=[C:11]3[C:15](=[C:16]([C:18]([NH2:20])=[O:19])[CH:17]=2)[NH:14][CH:13]=[C:12]3[CH:21]2[CH2:26][CH2:25][N:24]([S:27]([CH2:30][CH3:31])(=[O:29])=[O:28])[CH2:23][CH2:22]2)[CH:6]=[CH:7][CH:8]=1.[Cl:32][C:33]1[CH:38]=[CH:37][C:36]([Cl:39])=[CH:35][C:34]=1[S:40](Cl)(=[O:42])=[O:41].CCN(C(C)C)C(C)C>CN(C=O)C.C(Cl)Cl>[Cl:32][C:33]1[CH:38]=[CH:37][C:36]([Cl:39])=[CH:35][C:34]=1[S:40]([NH:1][CH2:2][C:3]1[CH:4]=[C:5]([C:9]2[CH:10]=[C:11]3[C:15](=[C:16]([C:18]([NH2:20])=[O:19])[CH:17]=2)[NH:14][CH:13]=[C:12]3[CH:21]2[CH2:22][CH2:23][N:24]([S:27]([CH2:30][CH3:31])(=[O:29])=[O:28])[CH2:25][CH2:26]2)[CH:6]=[CH:7][CH:8]=1)(=[O:42])=[O:41]

참가 물질

6

반응물 3

HCID 794012,5-Dichlorobenzenesulfonyl chlorideHCID 81531DiisopropylethylamineHCID 16038109HCID 16038109, 화합물

생성물 1

HCID 57732809HCID 57732809, 화합물수율 11%

시약·촉매·용매 2

HCID 6228Dimethylformamide용매HCID 6344Dichloromethane용매

실험 절차

To a solution of 5-[3-(aminomethyl)phenyl]-3-[1-(ethylsulfonyl)-4-piperidinyl]-1H-indole-7-carboxamide (40 mg, 0.096 mmol) in DMF (1.0 mL) and DCM (1.0 mL) was added 2,5-dichlorobenzenesulfonyl chloride (86 mg, 0.352 mmol) and DIEA (62 μL, 0.352 mmol). Reaction was stirred at room temperature for 6 h. Reaction mixture was then concentrated and purified by Gilson Preparatory HPLC to give 6.6 mg the title compound (11%).

후처리

  1. customReaction
  2. customReaction mixture
  3. concentrationwas then concentrated
  4. custompurified by Gilson Preparatory HPLC

출처 및 근거

ORD 기록
ord-ba76fe58e81d4f3bba2ab90f03b04001
출처 데이터셋
uspto-grants-2011_11
특허 번호
US08063071B2

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