Tang Hai-Tao, Xiong Kai, Li Ren-Hao, Ding Zong-Cang, Zhan Zhuang-Ping
Department of Chemistry, College of Chemistry and Chemical Engineering, Xiamen University , Xiamen, Fujian, People's Republic of China.
Org Lett. 2015 Jan 16;17(2):326-9. doi: 10.1021/ol503437n. Epub 2014 Dec 26.
An efficient method for the preparation of 5,6-dihydropyrazolo[1,5-c]quinazolines via gold(I)-catalyzed chemoselective bicyclization of N-propargylic sulfonylhydrazones has been developed. This process relies on the chemoselective cyclization of the hydrazone nitrogen instead of the usually favored aniline nitrogen onto the alkyne. The synthetic utility of the current strategy is demonstrated through the synthesis of a potential Eg5/Kinesin spindle protein inhibitor.
已开发出一种通过金（I）催化的N-炔丙基磺酰腙的化学选择性双环化反应制备5,6-二氢吡唑并[1,5-c]喹唑啉的有效方法。该过程依赖于腙氮而非通常更有利的苯胺氮对炔烃的化学选择性环化反应。通过合成一种潜在的Eg5/驱动蛋白纺锤体蛋白抑制剂，证明了当前策略的合成效用。
