Hydrazine hydrate (1:1) → 4-(4-cyclopropyl-1H-imidazol-1-yl)-N-(5-(hydrazinecarbonyl)thiophen-3-yl)picolinamide

HRID 2091615

반응식

HRID 2091615 반응식
[CH:1]1([C:4]2[N:5]=[CH:6][N:7]([C:9]3[CH:14]=[CH:13][N:12]=[C:11]([C:15]([NH:17][C:18]4[CH:19]=[C:20]([C:23](OC)=[O:24])[S:21][CH:22]=4)=[O:16])[CH:10]=3)[CH:8]=2)[CH2:3][CH2:2]1.O.[NH2:28][NH2:29]>C(O)C>[CH:1]1([C:4]2[N:5]=[CH:6][N:7]([C:9]3[CH:14]=[CH:13][N:12]=[C:11]([C:15]([NH:17][C:18]4[CH:19]=[C:20]([C:23]([NH:28][NH2:29])=[O:24])[S:21][CH:22]=4)=[O:16])[CH:10]=3)[CH:8]=2)[CH2:3][CH2:2]1

참가 물질

4

반응물 2

HCID 24654Hydrazine hydrate (1:1)HCID 58035644methyl 4-(4-(4-cyclopropyl-1H-imidazol-1-yl)picolinamido)thiophene-2-carboxylate

생성물 1

HCID 580356454-(4-cyclopropyl-1H-imidazol-1-yl)-N-(5-(hydrazinecarbonyl)thiophen-3-yl)picolinamide수율 103.1%

시약·촉매·용매 1

HCID 702Ethanol용매

실험 절차

Methyl 4-(4-(4-cyclopropyl-1H-imidazol-1-yl)picolinamido)thiophene-2-carboxylate (380 mg, 1.0 mmol) was dissolved in ethanol, hydrazine hydrate (0.26 mL, 5.2 mmol) was added, and the reaction was refluxed overnight. The solvent was removed under reduced pressure, and the solids were suspended in acetonitrile and filtered to afford 380 mg of 4-(4-cyclopropyl-1H-imidazol-1-yl)-N-(5-(hydrazinecarbonyl)thiophen-3-yl)picolinamide as a white solid. M+1=369.1

후처리

  1. temperaturethe reaction was refluxed overnight
  2. customThe solvent was removed under reduced pressure
  3. filtrationfiltered

출처 및 근거

ORD 기록
ord-8e94bcac882e46f39e04ba94b747e4e3
출처 데이터셋
uspto-grants-2013_05
특허 번호
US08440665B2

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