MASTPROM, WHI-P154

2-溴-4-(6,7-二甲氧基喹唑啉-4-基氨基)苯酚Chemical Name: 4-(3-Bromo-4-hydroxyphenylamino)-6,7-dimethoxyquinazoline; 2-Bromo-4-(6,7-dimethoxyquinazolin-4-ylamino)phenol
CAS No. 211555-04-3
项目整合开发状态: Preclinical
项目研究机构: Parker Hughes Institute
合成路线:4,5-Dimethoxy-2-nitrobenzoic acid (I) was treated with thionyl chloride to form acid chloride (II),followed by reaction with ammonia to yield 4,5-dimethoxy-2-nitrobenzamide (III).This was reduced with sodium borohydride in the presence of copper sulfate to give aminobenzamide (IV),which was refluxed with formic acid to afford 6,7-dimethoxyquinazoline-4(3H)-one (V).Subsequent treatment of (V) with phosphoryl chloride gave the chloroquinazoline (VI).The title compound was then prepared by condensation of (VI) with 2-bromo-4-aminophenol (VII) in refluxing ethanol.

合成路线:4,5-Dimethoxy-2-nitrobenzoic acid (I) was treated with thionyl chloride to form acid chloride (II),followed by reaction with ammonia to yield 4,5-dimethoxy-2-nitrobenzamide (III).This was reduced with sodium borohydride in the presence of copper sulfate to give aminobenzamide (IV),which was refluxed with formic acid to afford 6,7-dimethoxyquinazoline-4(3H)-one (V).Subsequent treatment of (V) with phosphoryl chloride gave the chloroquinazoline (VI).The title compound was then prepared by condensation of (VI) with 4-aminophenol (VII) in refluxing ethanol.