tert-butyl (4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)acetate hydrochloride → (4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)acetic acid

HRID 640008

반응식

HRID 640008 반응식
Cl.[Cl:2][CH2:3][CH2:4][CH2:5][O:6][C:7]1[CH:16]=[C:15]2[C:10]([C:11]([NH:17][C:18]3[CH:19]=[N:20][N:21]([CH2:23][C:24]([O:26]C(C)(C)C)=[O:25])[CH:22]=3)=[N:12][CH:13]=[N:14]2)=[CH:9][CH:8]=1>FC(F)(F)C(O)=O>[ClH:2].[Cl:2][CH2:3][CH2:4][CH2:5][O:6][C:7]1[CH:16]=[C:15]2[C:10]([C:11]([NH:17][C:18]3[CH:19]=[N:20][N:21]([CH2:23][C:24]([OH:26])=[O:25])[CH:22]=3)=[N:12][CH:13]=[N:14]2)=[CH:9][CH:8]=1

참가 물질

4

반응물 1

HCID 86609386tert-butyl (4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)acetate hydrochloride

생성물 2

HCID 313Hydrochloric AcidHCID 68638745(4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)acetic acid수율 197.1%

시약·촉매·용매 1

HCID 6422Trifluoroacetic acid용매

실험 절차

A solution of tert-butyl (4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)acetate hydrochloride (7.33 g, 16.1 mmol) in trifluoroacetic acid (60 ml) was stirred at room temperature for 30 minutes. The mixture was concentrated and the residue was suspended in water (120 ml), basified to pH 12 with 40% aqueous sodium hydroxide solution and then re-acidified to pH 4.8 with 2N aqueous hydrochloric acid to give (4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)acetic acid (5.74 g, 98% yield) as a cream coloured solid:

후처리

  1. concentrationThe mixture was concentrated

출처 및 근거

ORD 기록
ord-6d8fccfec7c9465697b7695f5e05a15e
출처 데이터셋
uspto-grants-2010_04
특허 번호
US07691867B2

연결된 노트

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