Synthesis of 5,6-Dihydropyrazolo[1,5-<i>c</i>]quinazolines through Gold-Catalyzed Chemoselective Bicyclization of <i>N</i>-Propargylic Sulfonylhydrazones
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
已经开发了一种通过金(I)催化的N-炔丙基磺酰基hydr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。该方法依赖于nitrogen氮的化学选择性环化,而不是通常偏向苯炔的苯胺氮。通过合成潜在的Eg5 / Kinesin纺锤体蛋白抑制剂,证明了当前策略的合成效用。