Methanol → 2-Oxo-3-benzoylamino-5-(3-phenylpropionyl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-1-acetic acid

HRID 1384724노트

반응식

HRID 1384724 반응식
C[O:2][C:3](=[O:36])[CH2:4][N:5]1[C:11]2[CH:12]=[CH:13][CH:14]=[CH:15][C:10]=2[N:9]([C:16](=[O:25])[CH2:17][CH2:18][C:19]2[CH:24]=[CH:23][CH:22]=[CH:21][CH:20]=2)[CH2:8][C@H:7]([NH:26][C:27](=[O:34])[C:28]2[CH:33]=[CH:32][CH:31]=[CH:30][CH:29]=2)[C:6]1=[O:35].CO.O.O[Li].O>C1COCC1>[O:35]=[C:6]1[N:5]([CH2:4][C:3]([OH:36])=[O:2])[C:11]2[CH:12]=[CH:13][CH:14]=[CH:15][C:10]=2[N:9]([C:16](=[O:25])[CH2:17][CH2:18][C:19]2[CH:20]=[CH:21][CH:22]=[CH:23][CH:24]=2)[CH2:8][CH:7]1[NH:26][C:27](=[O:34])[C:28]1[CH:29]=[CH:30][CH:31]=[CH:32][CH:33]=1

참가 물질

6

반응물 4

HCID 887MethanolHCID 962WaterHCID 168937Lithium hydroxide, monohydrateHCID 57159598(3S)-2-Oxo-3-benzoylamino-5-(3-phenylpropionyl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-1-acetic acid methyl ester

생성물 1

HCID 184659092-Oxo-3-benzoylamino-5-(3-phenylpropionyl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-1-acetic acid수율 19%

시약·촉매·용매 1

HCID 8028Tetrahydrofuran용매

실험 절차

(3S)-2-Oxo-3-benzoylamino-5-(3-phenylpropionyl)-2,3,4,5-tetrahydro-1H-1,5-benzo diazepine-1-acetic acid methyl ester (602a; 1.25 g, 2.57 mmol) was dissolved in 11 ml of THF, MeOH and H2O (5:5:1) and treated with LiOH.H2O (42 mg, 0.62 mmol) stirred at RT for 64 h. The reaction was concentrated in vacuo, diluted with H2O and acidified with aq. 1N HCl to give 230 mg of 603a as a white solid.

후처리

  1. concentrationThe reaction was concentrated in vacuo
  2. additiondiluted with H2O

출처 및 근거

ORD 기록
ord-9ef90fab98fe457fa3d78fe2d6258638
출처 데이터셋
uspto-grants-2001_07
특허 번호
US06258948B1

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