Pyridine → HCID 178449817, 화합물

HRID 1053623노트

반응식

HRID 1053623 반응식
[Cl:1][C:2]1[CH:3]=[C:4]([C:7]([N:9]([CH2:19][CH:20]2[CH2:23][CH2:22][CH2:21]2)[CH2:10][C:11]2[CH:16]=[CH:15][C:14]([OH:17])=[CH:13][C:12]=2[F:18])=[O:8])[NH:5]C=1.[C:24]([NH:31][C@:32]([C:36]([OH:38])=O)([CH3:35])[CH2:33][CH3:34])([O:26][C:27]([CH3:30])([CH3:29])[CH3:28])=[O:25].C1CCC([N:45]=C=NC2CCCCC2)CC1.N1C=CC=CC=1>C(OCC)(=O)C>[C:24]([NH:31][C@@:32]([CH3:35])([CH2:33][CH3:34])[C:36]([O:17][C:14]1[CH:15]=[CH:16][C:11]([CH2:10][N:9]([CH2:19][CH:20]2[CH2:21][CH2:22][CH2:23]2)[C:7]([C:4]2[NH:5][N:45]=[C:2]([Cl:1])[CH:3]=2)=[O:8])=[C:12]([F:18])[CH:13]=1)=[O:38])([O:26][C:27]([CH3:30])([CH3:29])[CH3:28])=[O:25]

참가 물질

6

반응물 4

HCID 1049PyridineHCID 10868DicyclohexylcarbodiimideHCID 14284791(R)-2-((tert-Butoxycarbonyl)amino)-2-methylbutanoic acidHCID 901023224-chloro-N-(cyclobutylmethyl)-N-(2-fluoro-4-hydroxybenzyl)-1H-pyrrole-2-carboxamide

생성물 1

HCID 178449817HCID 178449817, 화합물수율 0%

시약·촉매·용매 1

HCID 8857Ethyl Acetate용매

실험 절차

To a solution of 4-chloro-N-(cyclobutylmethyl)-N-(2-fluoro-4-hydroxybenzyl)-1H-pyrrole-2-carboxamide (0.040 g, 0.118 mmol) in 3 mL ethyl acetate was added Boc-iso-Valine (0.026 g, 0.118 mmol), DCC (0.037 g, 0.178 mmol) and pyridine 0.5 mL. The reaction mixture was added at r.t. for overnight. After removal of all the solvent, the residue was purified by chromatography. (0-30% methanol/DCM) (S)-4-((3-chloro-N-(cyclobutylmethyl)-1H-pyrazole-5-carboxamido)methyl)-3-fluorophenyl 2-(Boc-amino)-2-methylbutanoate was obtained (0.030 g, 0.056 mmol, 47% yield).

후처리

  1. additionThe reaction mixture was added at r.t. for overnight
  2. customAfter removal of all the solvent
  3. customthe residue was purified by chromatography

출처 및 근거

ORD 기록
ord-32d28061defe445d994651e37e6336f0
출처 데이터셋
uspto-grants-2016_07
특허 번호
US09394257B2

반응 노트

불러오는 중…