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Hydrochloric Acid → (S)-3-(4-bromo-2-fluoro-5-methylphenoxy)-1-(piperidin-4-yl)pyrrolidin-2-one hydrochloride

HRID 407985
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HRID 407985 반응식
[Br:1][C:2]1[C:27]([CH3:28])=[CH:26][C:5]([O:6][C@H:7]2[CH2:11][CH2:10][N:9]([CH:12]3[CH2:17][CH2:16][N:15](C(OC(C)(C)C)=O)[CH2:14][CH2:13]3)[C:8]2=[O:25])=[C:4]([F:29])[CH:3]=1.[ClH:30]>C(Cl)Cl.CO.O1CCOCC1>[ClH:30].[Br:1][C:2]1[C:27]([CH3:28])=[CH:26][C:5]([O:6][C@H:7]2[CH2:11][CH2:10][N:9]([CH:12]3[CH2:17][CH2:16][NH:15][CH2:14][CH2:13]3)[C:8]2=[O:25])=[C:4]([F:29])[CH:3]=1
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참가 물질

5

반응물 2

HCID 313Hydrochloric AcidHCID 86688115(S)-tert-butyl 4-(3-(4-bromo-2-fluoro-5-methylphenoxy)-2-oxopyrrolidin-1-yl)piperidine-1-carboxylate

생성물 1

HCID 67469732(S)-3-(4-bromo-2-fluoro-5-methylphenoxy)-1-(piperidin-4-yl)pyrrolidin-2-one hydrochloride수율 101%

시약·촉매·용매 2

HCID 312751,4-Dioxane용매HCID 21226129
Dichloromethane methanol
용매

실험 절차

(S)-tert-butyl 4-(3-(4-bromo-2-fluoro-5-methylphenoxy)-2-oxopyrrolidin-1-yl)piperidine-1-carboxylate (2.3 g, 4.9 mmol) was dissolved in CH2Cl2:MeOH (9:1, 50 mL). 4N HCl in dioxane (10 mL) was added and the reaction stirred at ambient temperature overnight. The reaction was concentrated to afford crude (S)-3-(4-bromo-2-fluoro-5-methylphenoxy)-1-(piperidin-4-yl)pyrrolidin-2-one hydrochloride (2.0 g, 4.9 mmol, 101% yield) which was used without further purification.

후처리

  1. concentrationThe reaction was concentrated

출처 및 근거

ORD 기록
ord-be615116b6e4465782f76a455804ff84
출처 데이터셋
uspto-grants-2014_06
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08754226B2

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