4-Methylmorpholine → (S)-1-(2-methoxy-5-(1H-tetrazol-1-yl)benzoyl)-3-(3,4-dichlorophenyl)-3-(2-methanesulfonyloxyethyl)pyrrolidine

HRID 343510노트

반응식

HRID 343510 반응식
[CH3:1][O:2][C:3]1[CH:26]=[CH:25][C:24]([N:27]2[CH:31]=[N:30][N:29]=[N:28]2)=[CH:23][C:4]=1[C:5]([N:7]1[CH2:11][CH2:10][C@@:9]([C:15]2[CH:20]=[CH:19][C:18]([Cl:21])=[C:17]([Cl:22])[CH:16]=2)([CH2:12][CH2:13][OH:14])[CH2:8]1)=[O:6].CN1CCOCC1.[CH3:39][S:40](Cl)(=[O:42])=[O:41]>C1(C)C=CC=CC=1>[CH3:1][O:2][C:3]1[CH:26]=[CH:25][C:24]([N:27]2[CH:31]=[N:30][N:29]=[N:28]2)=[CH:23][C:4]=1[C:5]([N:7]1[CH2:11][CH2:10][C@@:9]([C:15]2[CH:20]=[CH:19][C:18]([Cl:21])=[C:17]([Cl:22])[CH:16]=2)([CH2:12][CH2:13][O:14][S:40]([CH3:39])(=[O:42])=[O:41])[CH2:8]1)=[O:6]

참가 물질

5

반응물 3

HCID 79724-MethylmorpholineHCID 31297Methanesulfonyl chlorideHCID 53771624(S)-1-(2-methoxy-5-(1H-tetrazol-1-yl)benzoyl)-3-(3,4-dichlorophenyl)-3-(2-hydroxyethyl)pyrrolidine

생성물 1

HCID 53887278(S)-1-(2-methoxy-5-(1H-tetrazol-1-yl)benzoyl)-3-(3,4-dichlorophenyl)-3-(2-methanesulfonyloxyethyl)pyrrolidine

시약·촉매·용매 1

HCID 1140Toluene용매2회

실험 절차

Combine (S)-1-(2-methoxy-5-(1H-tetrazol-1-yl)benzoyl)-3-(3,4-dichlorophenyl)-3-(2-hydroxyethyl)pyrrolidine (200 mg, 0.44 mmol) and N-methylmorpholine (0.97 mmol) in toluene (10 mL). Add dropwise, methanesulfonyl chloride (0.066 g, 0.57 mmol). After 12 hours, dilute with toluene (20 mL) and extract with 1M hydrochloric acid solution and 5% sodium bicarbonate solution. Dry the organic layer over MgSO4, filter, and concentrate invacuo to give the title compound.

후처리

  1. additionAdd dropwise
  2. extractionextract with 1M hydrochloric acid solution and 5% sodium bicarbonate solution
  3. dry with materialDry the organic layer over MgSO4
  4. filtrationfilter
  5. concentrationconcentrate invacuo

출처 및 근거

ORD 기록
ord-da92492a1b3444258ec0bc6f1a31011a
출처 데이터셋
uspto-grants-1999_01
특허 번호
US05861417

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