Triethylamine → N-(5-((4-(hydroxymethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)methyl)-2,3-dihydro-1H-inden-1-yl)-2-methoxybenzenesulfonamide

HRID 43021

반응식

HRID 43021 반응식
[NH2:1][CH:2]1[C:10]2[C:5](=[CH:6][C:7]([CH2:11][N:12]3[CH:16]=[C:15]([CH2:17][OH:18])[C:14]([C:19]([F:22])([F:21])[F:20])=[N:13]3)=[CH:8][CH:9]=2)[CH2:4][CH2:3]1.C(N(CC)CC)C.[CH3:30][O:31][C:32]1[CH:37]=[CH:36][CH:35]=[CH:34][C:33]=1[S:38](Cl)(=[O:40])=[O:39]>C(Cl)Cl>[OH:18][CH2:17][C:15]1[C:14]([C:19]([F:22])([F:21])[F:20])=[N:13][N:12]([CH2:11][C:7]2[CH:6]=[C:5]3[C:10](=[CH:9][CH:8]=2)[CH:2]([NH:1][S:38]([C:33]2[CH:34]=[CH:35][CH:36]=[CH:37][C:32]=2[O:31][CH3:30])(=[O:40])=[O:39])[CH2:3][CH2:4]3)[CH:16]=1

참가 물질

5

반응물 3

HCID 8471TriethylamineHCID 37458512-Methoxybenzenesulfonyl ChlorideHCID 58230802(1-((1-Amino-2,3-dihydro-1H-inden-5-yl)methyl)-3-(trifluoromethyl)-1H-pyrazol-4-yl)methanol

생성물 1

HCID 53319053N-(5-((4-(hydroxymethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)methyl)-2,3-dihydro-1H-inden-1-yl)-2-methoxybenzenesulfonamide수율 28.1%

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

To a solution of (1-((1-amino-2,3-dihydro-1H-inden-5-yl)methyl)-3-(trifluoromethyl)-1H-pyrazol-4-yl)methanol (0.096 mmol, 30 mg) and triethylamine (0.193 mmol, 0.027 mL, 19.50 mg) in DCM (0.9 mL) was added 2-methoxybenzenesulfonyl chloride (0.096 mmol, 19.91 mg) and the whole stirred at room temperature for 3 h. The reaction mixture was concentrated under reduced pressure and the residue purified by RP-HPLC to give a white solid (13.0 mg, 0.027 mmol, 28%). [M+H]+ 482.2.

후처리

  1. concentrationThe reaction mixture was concentrated under reduced pressure
  2. customthe residue purified by RP-HPLC

출처 및 근거

ORD 기록
ord-a1b409fa8ebd44e5ab4a3d178de15525
출처 데이터셋
uspto-grants-2013_09
특허 번호
US08536214B2

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