Triethylamine → 5-(5-(((5-fluoro-2-oxoindolin-3-ylidene)hydrazono)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamido)-N-(2-amino-4-fluorophenyl)pentanamide

HRID 251662노트

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[F:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[NH:7][C:6](=[O:11])[C:5]2=[N:12][N:13]=[CH:14][C:15]1[NH:19][C:18]([CH3:20])=[C:17]([C:21]([NH:23][CH2:24][CH2:25][CH2:26][CH2:27][C:28](O)=[O:29])=[O:22])[C:16]=1[CH3:31].Cl.C(N=C=NCCCN(C)C)C.OC1C2N=NNC=2C=CC=1.C(N(CC)CC)C.[F:61][C:62]1[CH:67]=[CH:66][C:65]([NH2:68])=[C:64]([NH2:69])[CH:63]=1>[Cl-].[Na+].O.CN(C=O)C>[F:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[NH:7][C:6](=[O:11])[C:5]2=[N:12][N:13]=[CH:14][C:15]1[NH:19][C:18]([CH3:20])=[C:17]([C:21]([NH:23][CH2:24][CH2:25][CH2:26][CH2:27][C:28]([NH:68][C:65]2[CH:66]=[CH:67][C:62]([F:61])=[CH:63][C:64]=2[NH2:69])=[O:29])=[O:22])[C:16]=1[CH3:31]

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실험 절차

5-(5-(((5-fluoro-2-oxoindolin-3-ylidene)hydrazono)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamido)-pentanoic acid (427 mg, 1 mmol), and 8 ml of DMF were stirred at room temperature while 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (394 mg, 2 mmol), hydroxy-benzotriazole (162 mg, 1.2 mmol), triethylamine (404 mg, 4 mmol) and 4-fluoro-o-phenylenediamine (151 mg, 1.2 mmol) were added. The mixture was stirred for 24 hours at room temperature. The mixture was diluted with 400 mL of brine. The solids were collected by vacuum filtration, washed with water and dried under vacuum to give the title compound (439 mg, 82% yield) as a red solid. LC-MS (m/z) 536 (M+1).

후처리

additionwere added
filtrationThe solids were collected by vacuum filtration
washwashed with water
customdried under vacuum

출처 및 근거

ORD 기록: ord-9ed49a0782b040448b936b949cb31cfc
출처 데이터셋: uspto-grants-2011_01
DOI: 10.6084/m9.figshare.5104873.v1
특허 번호: US07863315B2

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생성물 1

시약·촉매·용매 2

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