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

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 Ⅱ_3～5 and Ⅱ₁₃ were found to increase the tolerance of mice to hypoxia. Further evaluation is in progress.

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

In order to search for effective antimyocardial ischemic agents, fourteen new 3-4-(3-alkylamino-2-hydroxy)propoxy]phenyl(benzyl)]-substituted 4(3H)-quinazolinones (II) were synthesized. Substituted o-aminobenzoic acids used as the starting materials were allowed to react with acetic anhydride and then p-amino-phenol (method A), or with N-(4-hydroxyphenyl)formamide (method B), or with thionyl chloride and then N-(4-hydroxybenzyl)formamide (method C) to form 3-(4-hydroxyphenyl(benzyl)]-substituted 4(3H)-quinazolinones (III). The intermediate III reacted with epichlorohydrin 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.