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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

史疆 地里夏提·白克力 张晨 鄂晓 尹东锋 王晓锋

中国药房2018,Vol.29Issue(6):746-749,4.
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

史疆 1地里夏提·白克力 1张晨 1鄂晓 1尹东锋 1王晓锋1

作者信息

  • 1. 新疆军区总医院药剂科,乌鲁木齐830000
  • 折叠

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

医药卫生

引用本文复制引用

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)

中国药房

OA北大核心CSTPCD

1001-0408

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