摘要
哌嗪、吗啉是小分子药物中常见的结构片段,2,6-二氮杂螺[3,4]环辛烷和2-氧-6-氮杂螺[3,4]环辛烷等四元螺环化合物作为其类似物,在药物化学领域具有良好的应用前景.本研究以廉价易得的丙二酸二乙酯或丙烯酸乙酯为起始原料,经[3+2]环加成反应,可便捷高效地完成6-苄基-2,6-二氮杂螺[3,4]环辛烷和2-氧-6-氮杂螺[3,4]环辛烷克级水平的合成.
Piperazine and morpholine are common modules in drugs. Design and synthesis of their surrogates may help to explore the chemical and patent space in medicinal chemistry. In this article, through [3 q-2] cycloaddition, the improved syn- thesis of 6-benzyl-2,6-diazaspiro[3.4]octane oxalate and 2-oxa-6-azaspiro[3.4]octane as substitutes of piperazine and morpholine was provided, respectively. Multi-gram quantities of the compounds could be easily obtained in relatively high yields.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2015年第1期137-143,共7页
Chinese Journal of Organic Chemistry
基金
教育部博士点基金(No.20130071110071)
上海市自然科学基金(No.12ZR1403300)
上海市科技支撑(No.13431900102)资助项目~~