CAJ | 학술논문

以2-氨基-5-碘苯甲酸与醋酸脒反应制得6-碘喹唑啉-4-酚,再以三光气（BTC）为氯化试剂,DMF为催化剂,BTC与6-碘喹唑啉-4-酚的投料比为1.1∶3,二氯甲烷为溶剂,于40℃下反应2.5 h,得到抗癌药拉帕替尼的关键中间体4-氯-6-碘喹唑啉,收率78%。工艺具有条件温和,后处理简单,对环境友好等特点。
이2-안기-5-전분갑산여작산미반응제득6-전규서람-4-분,재이삼광기（BTC）위록화시제,DMF위최화제,BTC여6-전규서람-4-분적투료비위1.1∶3,이록갑완위용제,우40℃하반응2.5 h,득도항암약랍파체니적관건중간체4-록-6-전규서람,수솔78%。공예구유조건온화,후처리간단,대배경우호등특점。
6-iodoquinazolin-4-ol was synthesized from 2-chloro-5-iodobenzoic acid and formamidine acetate,which was then followed by chlorination using triphosgene as chlorinating reagent catalyzed by DMF in dichloromethane at 40 ℃ for 2.5 h to obtain the key intermediate 4-chloro-6-idioquinazoline of antitumor agent lapatini.The overall yield was 78 %.The process was characterized by mild reaction conditions,simple operation and environmental benign.