1-Piperazinecarboxylic acid, ethyl ester → 2-(4-Carbethoxypiperazin-1-yl)-4-amino-6,7-dimethoxyquinazoline

HRID 461332ノート

反応式

HRID 461332 の反応式
[NH2:1][C:2]1[C:11]2[C:6](=[CH:7][C:8]([O:14][CH3:15])=[C:9]([O:12][CH3:13])[CH:10]=2)[N:5]=[C:4](Cl)[N:3]=1.[CH3:17][CH2:18][O:19][C:20]([N:22]1[CH2:27][CH2:26][NH:25][CH2:24][CH2:23]1)=[O:21]>>[C:20]([N:22]1[CH2:27][CH2:26][N:25]([C:4]2[N:3]=[C:2]([NH2:1])[C:11]3[C:6](=[CH:7][C:8]([O:14][CH3:15])=[C:9]([O:12][CH3:13])[CH:10]=3)[N:5]=2)[CH2:24][CH2:23]1)([O:19][CH2:18][CH3:17])=[O:21]

参加物

3

反応物 2

HCID 84311-Piperazinecarboxylic acid, ethyl esterHCID 902352-Chloro-6,7-dimethoxy-4-quinazolinamine

生成物 1

HCID 133706732-(4-Carbethoxypiperazin-1-yl)-4-amino-6,7-dimethoxyquinazoline

反応条件

温度
100 °C

実験手順

In a reaction vessel equipped with stirrer, thermometer and drying tube was charged 60 ml. of isoamyl alcohol, 10 g. (0.042 mole) of 4-amino-2-chloro-6,7-dimethoxyquinazoline (prepared as described in U.S. Pat. No. 3,511,836) and 7.3 g. (0.047 mole) ethyl-N-piperazinocarboxylate (Aldrich Chemical Co.). The mixture was heated at 100° C. for 3 hours and allowed to stand overnight at room temperature. The mixture was diluted with 120 ml. of isoamyl alcohol and filtered to obtain 14.3 g. (94%) of the hydrochloride salt of the title compound, which melted sharply at 295° C.

後処理

  1. customIn a reaction vessel equipped with stirrer
  2. customthermometer and drying tube
  3. additionwas charged 60 ml
  4. additionThe mixture was diluted with 120 ml
  5. filtrationof isoamyl alcohol and filtered
  6. customto obtain 14.3 g

出典と根拠

ORDレコード
ord-7b4e09c206f44fffa65c05624613a57d
出典データセット
uspto-grants-1977_12
特許番号
US04062844

反応ノート

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