2,6-Diethylaniline → 8-Amino-N-(2,6-diethylphenyl)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide

HRID 81950

反応式

HRID 81950 の反応式
[NH2:1][C:2]1[N:11]=[CH:10][C:9]2[CH2:8][CH2:7][C:6]3[C:12]([C:16]([OH:18])=O)=[N:13][N:14]([CH3:15])[C:5]=3[C:4]=2[N:3]=1.[K].C(N(C(C)C)C(C)C)C.ON1C2C=CC=CC=2N=N1.[CH2:39]([C:41]1[CH:47]=[CH:46][CH:45]=[C:44]([CH2:48][CH3:49])[C:42]=1[NH2:43])[CH3:40]>CN(C)C=O.O>[NH2:1][C:2]1[N:11]=[CH:10][C:9]2[CH2:8][CH2:7][C:6]3[C:12]([C:16]([NH:43][C:42]4[C:44]([CH2:48][CH3:49])=[CH:45][CH:46]=[CH:47][C:41]=4[CH2:39][CH3:40])=[O:18])=[N:13][N:14]([CH3:15])[C:5]=3[C:4]=2[N:3]=1

参加物

7

反応物 4

HCID 113692,6-DiethylanilineHCID 757711-HydroxybenzotriazoleHCID 81531DiisopropylethylamineHCID 67076100potassium 8-amino-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid

生成物 1

HCID 670756638-Amino-N-(2,6-diethylphenyl)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide収率 70%

試薬・触媒・溶媒 2

HCID 962Water溶媒HCID 6228Dimethylformamide溶媒

実験手順

A suspension of potassium 8-amino-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid (180 mg, 0.73 mmol) in anhydrous dimethylformamide (5.0 mL) was treated with N-ethyl-N,N-diisopropylamine (0.258 mL, 1.47 mmol) and N-ethyl-N′,N′-diisopropyl carbodiimide hydrochloride (EDCI) (280 mg, 1.47 mmol) and 1-hydroxybenzotriazole (200 mg, 1.47 mmol). The mixture was then treated with 2,6-diethylaniline (0.170 mL, 1.1 mmol). The reaction was stirred at room temperature overnight. The reaction was diluted with water and the resulting precipitate was collected by filtration to afford the title compound (190 mg, 70% yield).

後処理

  1. filtrationthe resulting precipitate was collected by filtration

出典と根拠

ORDレコード
ord-e607a4f63824469db74a4ab864200bfa
出典データセット
uspto-grants-2014_09
特許番号
US08846701B2

関連ノート

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