蔡玉春, 董永明. 抗心肌缺血药3-4-(2-羟基-3-烷氨基)丙氧基苯基(苄基)-取代4(3H)-喹唑酮的合成J. 药学学报, 1990, 25(11): 862-865.
引用本文: 蔡玉春, 董永明. 抗心肌缺血药3-4-(2-羟基-3-烷氨基)丙氧基苯基(苄基)-取代4(3H)-喹唑酮的合成J. 药学学报, 1990, 25(11): 862-865.
YC Cai, YM Dong. SYNTHESIS OF 3-4-(3-ALKYLAMINO-2-HYDROXY) PROPOXY PHENYL (BENZYL) - SUBSTITUTED 4(3H)-QUINAZOLINONES AS ANTIMYOCARDIAL ISCHEMIC AGENTSJ. Acta Pharmaceutica Sinica, 1990, 25(11): 862-865.
Citation: YC Cai, YM Dong. SYNTHESIS OF 3-4-(3-ALKYLAMINO-2-HYDROXY) PROPOXY PHENYL (BENZYL) - SUBSTITUTED 4(3H)-QUINAZOLINONES AS ANTIMYOCARDIAL ISCHEMIC AGENTSJ. Acta Pharmaceutica Sinica, 1990, 25(11): 862-865.

抗心肌缺血药3-4-(2-羟基-3-烷氨基)丙氧基苯基(苄基)-取代4(3H)-喹唑酮的合成

SYNTHESIS OF 3-4-(3-ALKYLAMINO-2-HYDROXY) PROPOXY PHENYL (BENZYL) - SUBSTITUTED 4(3H)-QUINAZOLINONES AS ANTIMYOCARDIAL ISCHEMIC AGENTS

  • Abstract: In order to search for effective antimyocardial ischemic agents, fourteen new 3 4-(3-alkylamino-2-hydroxy)propoxy phenyl(benzyl)-substituted 4(3H)-quin zolinones (Ⅱ) were synthesized. Substituted o-aminobenzoic acids used as the starting materials were allowed to react with acetic anhydride and then p-aminophenol (method A), or with N- (4- hydroxyphenyl)formamide (method B), or with thionyl chloride and then N - (4 - hydroxybenzyl) formamide (methode C) to form 3-(4-hydroxyphenyl(benzyl)-substituted 4(3H)-quinazolinones (Ⅲ). The intermediate Ⅲ reacted with epichiorohydrin to form the epoxides (Ⅳ). The reaction of Ⅳ with an excess of isopropylamine or tert-butylamine in boiling chloroform gave the desired products. Of all the compounds synthesized, Compounds Ⅱ3~5 and Ⅱ13 were found to increase the tolerance of mice to hypoxia. Further evaluation is in progress.

     

/

返回文章
返回