一类特殊的分子内类Aldol反应产物他达拉非有关物质E的合成研究
收稿日期: 2016-02-26
修回日期: 2016-04-12
网络出版日期: 2016-04-20
基金资助
国家自然科学基金(No. 21202112)、教育部博士点基金新教师类项目(20123201120019)、江苏高校优势学科建设工程资助项目.
Discovery of a Special Intramolecular Aldol-Like Reaction in the Synthesis of Related Substance E of Tadalafil
Received date: 2016-02-26
Revised date: 2016-04-12
Online published: 2016-04-20
Supported by
Project supported by the National Natural Science Foundation of China (Grant No.21202112), Ph.D. Programs Foundation of Ministry of Education of China (No. 20123201120019) and PAPD (A Project Funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions).
钱彭飞 , 万惠新 , 蒋静 , 胡延维 , 陈晓蓓 , 张士磊 . 一类特殊的分子内类Aldol反应产物他达拉非有关物质E的合成研究[J]. 有机化学, 2016 , 36(8) : 1878 -1882 . DOI: 10.6023/cjoc201602028
In the synthesis of related substance E of tadalafil, a special intramolecular aldol-like reaction was discovered. In this reaction, the α-carbon of ketone attacks the carbonyl group of amide, forming a stable amino hemiketal structure. This reaction can only be realized under the catalysis of silica gel, and other acidic or basic reaction conditions are difficult to obtain the desired product. This finding is a meaningful supplement and extension to aldol reactions.
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