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6-溴甲基 - 3,4-二氢 - 2 -甲基 - 4-氧代喹唑啉 ( 1 )是治疗结直肠癌一线药物 [1]雷替曲塞的重要中间体。本文参考文献以间甲苯甲酸 ( 2 )为原料经硝化 [2 ] 、还原[3 ] 、成环 [4 ] 和溴代 [5] 反应制得 1。硝化反应中产物 2 -硝基 - 5-甲基苯甲酸 ( 3)和副产物 3-甲基 -4-硝
6-Bromomethyl-3,4-dihydro-2-methyl-4-oxoquinazoline (1) is an important intermediate for the treatment of raltitrexed in first-line colorectal cancer [1]. The references in this paper were prepared by the reaction of m-toluic acid (2) with nitration [2], reduction [3], cyclization [4] and bromination [5] Nitration of 2-nitro-5-methylbenzoic acid (3) and by-product 3-methyl-4-