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p-Toluenesulfonic acid monohydrate → (3S)-3-Fluoropyrrolidine 4-methylbenzenesulfonate

HRID 1445772
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인쇄 미리보기

반응식

HRID 1445772 반응식
O.[C:2]1([CH3:12])[CH:7]=[CH:6][C:5]([S:8]([OH:11])(=[O:10])=[O:9])=[CH:4][CH:3]=1.[F:13][C@H:14]1[CH2:18][CH2:17][N:16](C(OC(C)(C)C)=O)[CH2:15]1>C(O)C>[CH3:12][C:2]1[CH:3]=[CH:4][C:5]([S:8]([OH:11])(=[O:10])=[O:9])=[CH:6][CH:7]=1.[F:13][C@H:14]1[CH2:18][CH2:17][NH:16][CH2:15]1
참가 물질실험 절차후처리출처 및 근거반응 노트

참가 물질

4

반응물 2

HCID 521998p-Toluenesulfonic acid monohydrateHCID 18453464tert-Butyl (3S)-3-fluoropyrrolidine-1-carboxylate2회

생성물 1

HCID 86614633(3S)-3-Fluoropyrrolidine 4-methylbenzenesulfonate수율 94.2%

시약·촉매·용매 1

HCID 702Ethanol용매

실험 절차

Add p-toluenesulfonic acid monohydrate (0.50 g, 2.64 mmol) to tert-butyl (3S)-3-fluoropyrrolidine-1-carboxylate (See Intermediate 48) (0.50 g, 2.64 mmol) in ethanol (5 mL) at room temperature. Stir the resulting solution overnight. Concentrate the reaction mixture in vacuo to remove solvent and bi-products to give the title compound as an off-white solid (0.65 g): MS (m/e): 90 (M+1).

후처리

  1. concentrationConcentrate the reaction mixture in vacuo
  2. customto remove solvent and bi-products

출처 및 근거

ORD 기록
ord-4ef1691e546240c894db82db09b1382f
출처 데이터셋
uspto-grants-2010_02
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07666871B2

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