4-氨基-2-氯-6,7-二甲氧基喹唑啉的合成

Synthesis of 4-Amino-2-chloro-6,7-dimethoxyquinazoline

香草醛经甲基化、硝化、氧化、酯化、还原、环合、氯化及氨化制得盐酸特拉唑嗪等喹唑啉类药物的中间体4-氨基-2-氯-6,7-二甲氧基喹唑啉,并考察了硝化、氧化过程中反应温度和投料比等因素对反应的影响,确立了最佳工艺条件,总收率约37%。

4-Amino-2-chloro-6,7-dimethoxyquinazoline,a key intermediate of quinazoline drugs such as terazosin,was synthesized from vanillin by methylation,nitration,oxidation,esterification,reduction,cyclization, chlorination and animation.The effects of reaction temperature and mole ratio of the reactants were investigated in the nitration and oxidation.The overall yield of the target compound was about 37%after improvement of the process.