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Hydrochloric Acid → 4-((1R,2R)-2-((3-fluoro-4-(1H-tetrazol-1-yl)benzyloxy)methyl)cyclopropyl)piperidinium chloride

HRID 1468870
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HRID 1468870 반응식
[ClH:1].O1CCOCC1.[F:8][C:9]1[CH:10]=[C:11]([CH:31]=[CH:32][C:33]=1[N:34]1[CH:38]=[N:37][N:36]=[N:35]1)[CH2:12][O:13][CH2:14][C@@H:15]1[CH2:17][C@@H:16]1[CH:18]1[CH2:23][CH2:22][N:21](C(OC(C)(C)C)=O)[CH2:20][CH2:19]1>C(Cl)Cl>[Cl-:1].[F:8][C:9]1[CH:10]=[C:11]([CH:31]=[CH:32][C:33]=1[N:34]1[CH:38]=[N:37][N:36]=[N:35]1)[CH2:12][O:13][CH2:14][C@@H:15]1[CH2:17][C@@H:16]1[CH:18]1[CH2:23][CH2:22][NH2+:21][CH2:20][CH2:19]1
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참가 물질

5

반응물 3

HCID 313Hydrochloric AcidHCID 312751,4-DioxaneHCID 71140737tert-butyl 4-((1R,2R)-2-((3-fluoro-4-(1H-tetrazol-1-yl)benzyloxy)methyl)cyclopropyl)piperidine-1-carboxylate

생성물 1

HCID 711160804-((1R,2R)-2-((3-fluoro-4-(1H-tetrazol-1-yl)benzyloxy)methyl)cyclopropyl)piperidinium chloride수율 99%

시약·촉매·용매 1

HCID 6344
Dichloromethane
용매

실험 절차

A solution of 4 M HCl in dioxane (2.4 mL, 9.62 mmol) was added to a solution of tert-butyl 4-((1R,2R)-2-((3-fluoro-4-(1H-tetrazol-1-yl)benzyloxy)methyl)cyclopropyl)piperidine-1-carboxylate (Step C product, 415 mg, 0.962 mmol) in DCM (3 mL). This mixture was stirred at rt for 1 hr. The reaction mixture was subsequently concentrated under reduced pressure to afford the title compound (351 mg, 99%) as a crude product to be used for the next step. LC/MS (m/z): 332 (M+H)+.

후처리

  1. concentrationThe reaction mixture was subsequently concentrated under reduced pressure

출처 및 근거

ORD 기록
ord-3c1a9ab6816d46c598f321a64c7992e6
출처 데이터셋
uspto-grants-2015_04
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US09006228B2

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