2-Amino-4,6-dimethoxypyrimidine → 4-(Cyclopropylcarbonyl)-N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-1-methyl-1H-pyrazole-5-sulfonamide

HRID 231405

反応式

HRID 231405 の反応式
[CH:1]1([C:4]([C:6]2[CH:7]=[N:8][N:9]([CH3:15])[C:10]=2[S:11]([NH2:14])(=[O:13])=[O:12])=[O:5])[CH2:3][CH2:2]1.C1(N[C:23](=O)[O-:24])C=CC=CC=1.[CH3:26][O:27][C:28]1[CH:33]=[C:32]([O:34][CH3:35])[N:31]=[C:30]([NH2:36])[N:29]=1.[N+](=C1CCCCCCCCCC1C1CCCCCCCCCC1)=[N-]>C(#N)C>[CH:1]1([C:4]([C:6]2[CH:7]=[N:8][N:9]([CH3:15])[C:10]=2[S:11]([NH:14][C:23]([NH:36][C:30]2[N:31]=[C:32]([O:34][CH3:35])[CH:33]=[C:28]([O:27][CH3:26])[N:29]=2)=[O:24])(=[O:13])=[O:12])=[O:5])[CH2:2][CH2:3]1

参加物

6

反応物 4

HCID 1189462-Amino-4,6-dimethoxypyrimidineHCID 142309984-Cyclopropylcarbonyl-1-methyl-5-pyrazolesulfonamideHCID 21896570PhenylcarbamateHCID 22171225HCID 22171225、化合物

生成物 1

HCID 142309994-(Cyclopropylcarbonyl)-N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-1-methyl-1H-pyrazole-5-sulfonamide

試薬・触媒・溶媒 1

HCID 6342Acetonitrile溶媒

実験手順

To a stirring mixture of the sulfonamide from Example 2 (175 mg, 0.76 mmol) and the phenylcarbamate of 4,6-dimethoxy-2-aminopyrimidine (210 mg, 0.76 mmol) in 3 ml of acetonitrile was added diazobicycloundecane (116 mg, 0.76 mmol). The solution was stirred for approximately 10 minutes. Acidification of the reaction mixture and filtration of the resulting solids afforded 300 mg of the desired compound m.p. 189°-192° C. NMR (200 MHz, CDCl3) 1.0 (m, 2H), 1.1 (m, 2H), 2.4 (m, 1H), 4.0 (s, 6H), 4.35 (s, 1H), 5.80 (s, 1H), 7.4 (br. s, 1H), 8.05 (s, 1H), 12.9 (s, 1H).

後処理

  1. filtrationAcidification of the reaction mixture and filtration of the resulting solids

出典と根拠

ORDレコード
ord-5b8f307d02064ce6995a15186cec2310
出典データセット
uspto-grants-1989_07
特許番号
US04846878

関連ノート

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