Dimethylformamide → N-{2-fluoro-5-[(2-{[(methoxyamino)carbonyl]amino}imidazo[1,2-b]pyridazin-6-yl)oxy]phenyl}-1,3-dimethyl-1H-pyrazole-5-carboxamide

HRID 1668022

반응식

Cl.[NH2:2][C:3]1[N:4]=[C:5]2[CH:10]=[CH:9][C:8]([O:11][C:12]3[CH:13]=[CH:14][C:15]([F:28])=[C:16]([NH:18][C:19]([C:21]4[N:25]([CH3:26])[N:24]=[C:23]([CH3:27])[CH:22]=4)=[O:20])[CH:17]=3)=[N:7][N:6]2[CH:29]=1.[Cl-].[CH3:31][O:32][NH3+:33].C(N(CC)CC)C.CN(C)[CH:43]=[O:44]>>[F:28][C:15]1[CH:14]=[CH:13][C:12]([O:11][C:8]2[CH:9]=[CH:10][C:5]3[N:6]([CH:29]=[C:3]([NH:2][C:43]([NH:33][O:32][CH3:31])=[O:44])[N:4]=3)[N:7]=2)=[CH:17][C:16]=1[NH:18][C:19]([C:21]1[N:25]([CH3:26])[N:24]=[C:23]([CH3:27])[CH:22]=1)=[O:20]

참가 물질

반응물 4

HCID 6228Dimethylformamide

HCID 8471Triethylamine

HCID 11639O-methylhydroxylammonium chloride

HCID 57505567N-{5-[(2-aminoimidazo[1,2-b]pyridazin-6-yl)oxy]-2-fluorophenyl}-1,3-dimethyl-1H-pyrazole-5-carboxamide hydrochloride

생성물 1

HCID 57505572N-{2-fluoro-5-[(2-{[(methoxyamino)carbonyl]amino}imidazo[1,2-b]pyridazin-6-yl)oxy]phenyl}-1,3-dimethyl-1H-pyrazole-5-carboxamide수율 54%

실험 절차

Using N-{5-[(2-aminoimidazo[1,2-b]pyridazin-6-yl)oxy]-2-fluorophenyl}-1,3-dimethyl-1H-pyrazole-5-carboxamide hydrochloride (200 mg, 0.48 mmol), 1,1′-carbonylimidazole (233 mg, 1.44 mmol), O-methylhydroxyammonium chloride (120 mg, 1.44 mmol), triethylamine (0.27 mL, 1.92 mmol) and N,N-dimethylformamide (6.0 mL), and by a reaction in the same manner as in Example 200, the title compound (117 mg, 54%) was obtained as pale-yellow crystals.

후처리

customby a reaction in the same manner as in Example 200

출처 및 근거

ORD 기록: ord-0dc4ce867ea94accaad44b5596fa53cf
출처 데이터셋: uspto-grants-2011_10
DOI: 10.6084/m9.figshare.5104873.v1
특허 번호: US08044049B2

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