河北师范大学学报—

期刊信息

刊名：河北师范大学学报（自然科学版）Journal of Hebei Normal University (Natural Science)
主办：河北师范大学
ISSN： 1000-5854
CN： 13-1061/N
中国科技核心期刊
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中国高校优秀科技期刊
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ABCA1和SR-B1双重基因上调表达剂5242331的合成

田文华¹

姜珊¹

许艳妮²

李文燕¹

(1.河北师范大学化学与材料科学学院，河北石家庄 050024; 2.中国医学科学院医药生物技术研究所，国家新药 (微生物) 筛选实验室，北京 100050)
DOI： 10.13763/j.cnki.jhebnu.nse.202103020

Synthesis of ABCA1 and SR-B1 Dual Expression Upregulator 5242331

TIAN Wenhua¹,JIANG Shan¹,XU Yanni²,LI Wenyan¹

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摘要/Abstract

摘要：

苯并噻唑类化合物5242331是通过高通量筛选得到的小分子ABCA1和SR-B1双重基因上调表达剂，具有较好的抗动脉粥样硬化作用. 以4-正丁基苯胺为原料，环合得到2-氨基-6-丁基苯并噻唑中间体1，3-氨基丙腈与4-氯磺酰基苯甲酸酰化得到4-[(N-氰乙基)氨磺酰基] 苯甲酸中间体2，再与中间体1缩合合成了化合物5242331，收率为71.6 %.

Abstract：

Benzothiazole 5242331 is an ABCA1 and SR-B1 dual expression upregulator obtained through high-throughput screening, which has a good anti-atherosclerosis effect. In this paper, 2-amino-6-butyl benzothiazole intermediate 1 was synthesized from The 4-n-butylaniline by cyclization. The 4-(N-(2-cyanoethyl)sulfamoyl)benzoic acid intermediate 2 was obtained by acylation 3-aminopropionitrile with 4-(chlorosulfonyl)benzoic acid. The target compound 5242331 was get by condensation of intermediates 1 and 2 in a yield of 71.6 %.

关键词

关键词： 5242331； ABCA1； SR-B1；双重基因上调表达剂；合成

Key words： 5242331 ; ABCA1 ; SR-B1 ; dual expression upregulator ; synthesis

参考文献 19

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