Metal-free synthesis of 1,4-benzodiazepines and quinazolinones from hexafluoroisopropyl 2-aminobenzoates at room temperature

被引:7
|
作者
Chen, Jiewen [1 ]
Liang, En [1 ]
Shi, Jie [1 ]
Wu, Yinrong [1 ]
Wen, Kangmei [1 ]
Yao, Xingang [1 ]
Tang, Xiaodong [1 ]
机构
[1] Southern Med Univ, Guangdong Prov Key Lab New Drug Screening, Sch Pharmaceut Sci, 1023 South Shatai Rd, Guangzhou 510515, Peoples R China
基金
中国国家自然科学基金;
关键词
ONE-POT SYNTHESIS; AMINO-ACID ESTERS; CASCADE SYNTHESIS; OXIDATIVE SYNTHESIS; O-AMINOBENZAMIDES; TANDEM; QUINAZOLIN-4(3H)-ONES; CONDENSATION; DERIVATIVES; PHARMACOKINETICS;
D O I
10.1039/d1ra00324k
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Herein, we describe the novel reactivity of hexafluoroisopropyl 2-aminobenzoates. The metal-free synthesis of 1,4-benzodiazepines and quinazolinones from hexafluoroisopropyl 2-aminobenzoates has been developed at room temperature. These procedures feature good functional group tolerance, mild reaction conditions, and excellent yields. The newly formed products can readily be converted to other useful N-heterocycles. Moreover, the products and their derivatives showed potent anticancer activities in vitro by MTT assay.
引用
收藏
页码:4966 / 4970
页数:5
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