中国药房2018,Vol.29Issue(6):746-749,4.DOI:10.6039/j.issn.1001-0408.2018.06.06
7-甲氧基-4-(2-甲基-4-喹唑啉基)-3,4-二氢喹噁啉-2(1H)-酮的合成工艺改进
Improvement of the Synthesis Technology of 7-methoxy-4-(2-methyl-4-quinazolinyl)-3,4-dihydroquinoxalin-2 (1H)-ketone
摘要
Abstract
OBJECTIVE:To improve the synthesis technology of 7-methoxy-4-(2-methyl-4-quinazolinyl)-3,4-dihydroquinoxalin-2 (1H)-ketone. METHODS:Using 2-methyl-4(3H)-quinazolone as starting material,the synthesis technology of 7-methoxy-4-(2-methyl-4-quinazolinyl)-3,4-dihydroquinoxalin-2(1H)-ketone was improved by clorination, nucleophilic substitution, diarylamine alkylation and nitro reductive cyclization. The yield of it was investigated. RESULTS:The structure of 7-methoxy-4-(2-methyl-4-quinazolinyl)-3,4-dihydroquinoxalin-2(1H)-ketone had been verified by 1H-NMR and ESI-MS. The yield was 43.5%and improved by 23.3% compared to 20.2% before improvement. CONCLUSIONS:Improved technology is simpler and milder, which is suitable for the batch preparation of laboratory study.关键词
7-甲氧基-4-(2-甲基-4-喹唑啉基)-3,4-二氢喹噁啉-2(1H)-酮/合成工艺/2-甲基-4(3H)-喹唑啉酮/改进Key words
7-methoxy-4-(2-methyl-4-quinazolinyl)-3/4-dihydroquinoxalin-2(1H)-ketone/Synthesis technology/2-methyl-4 (3H)-quinazolone/Improvement分类
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史疆,地里夏提·白克力,张晨,鄂晓,尹东锋,王晓锋..7-甲氧基-4-(2-甲基-4-喹唑啉基)-3,4-二氢喹噁啉-2(1H)-酮的合成工艺改进[J].中国药房,2018,29(6):746-749,4.基金项目
新疆维吾尔自治区自然科学基金面上项目(No.2015211C239) (No.2015211C239)