3-Hydroxyisovaleric acid → N-[5-({2-[(3-hydroxy-3-methylbutanoyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide

HRID 2391410

反応式

HRID 2391410 の反応式
[OH:1][C:2]([CH3:8])([CH3:7])[CH2:3][C:4]([OH:6])=O.Cl.[NH2:10][C:11]1[N:12]=[C:13]2[CH:18]=[CH:17][C:16]([O:19][C:20]3[CH:21]=[CH:22][C:23]([CH3:36])=[C:24]([NH:26][C:27]([C:29]4[N:33]([CH3:34])[N:32]=[C:31]([CH3:35])[CH:30]=4)=[O:28])[CH:25]=3)=[N:15][N:14]2[CH:37]=1.F[P-](F)(F)(F)(F)F.N1(OC(N(C)C)=[N+](C)C)C2N=CC=CC=2N=N1.C(N(CC)C(C)C)(C)C>CN(C)C=O>[OH:1][C:2]([CH3:8])([CH3:7])[CH2:3][C:4]([NH:10][C:11]1[N:12]=[C:13]2[CH:18]=[CH:17][C:16]([O:19][C:20]3[CH:21]=[CH:22][C:23]([CH3:36])=[C:24]([NH:26][C:27]([C:29]4[N:33]([CH3:34])[N:32]=[C:31]([CH3:35])[CH:30]=4)=[O:28])[CH:25]=3)=[N:15][N:14]2[CH:37]=1)=[O:6]

参加物

6

反応物 4

HCID 693623-Hydroxyisovaleric acidHCID 81531DiisopropylethylamineHCID 9886157Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 57505635N-{5-[(2-aminoimidazo[1,2-b]pyridazin-6-yl)oxy]-2-methylphenyl)-1,3-dimethyl-1H-pyrazole-5-carboxamide hydrochloride

生成物 1

HCID 57505650N-[5-({2-[(3-hydroxy-3-methylbutanoyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide収率 66%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

In the same manner as in Example 278 and using 3-hydroxy-3-methylbutanoic acid (74 mg, 0.63 mmol), N-{5-[(2-aminoimidazo[1,2-b]pyridazin-6-yl)oxy]-2-methylphenyl}-1,3-dimethyl-1H-pyrazole-5-carboxamide hydrochloride (200 mg, 0.48 mmol), O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate (240 mg, 0.63 mmol), N,N-diisopropylethylamine (190 mg, 1.5 mmol) and N,N-dimethylformamide (7 mL) as starting materials, the title compound (150 mg, 66%) was obtained as a pale-yellow solid.

出典と根拠

ORDレコード
ord-a07acad73eca4f72980ae8c8bf599987
出典データセット
uspto-grants-2012_09
特許番号
US08273741B2

関連ノート

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