title: Synthesis of 5,6-dihydropyrazolo[1,5-c]quinazolines through gold-catalyzed chemoselective bicyclization of N-propargylic sulfonylhydrazones.
abstract: 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.
authors.affiliation: Department of Chemistry, College of Chemistry and Chemical Engineering, Xiamen University , Xiamen, Fujian, People's Republic of China.
authors.forename: Hai-Tao
authors.initials: HT
authors.lastname: Tang
authors.forename: Kai
authors.initials: K
authors.lastname: Xiong
authors.forename: Ren-Hao
authors.initials: RH
authors.lastname: Li
authors.forename: Zong-Cang
authors.initials: ZC
authors.lastname: Ding
authors.forename: Zhuang-Ping
authors.initials: ZP
authors.lastname: Zhan
mesh_terms: D002384:Catalysis; D003500:Cyclization; D006046:Gold / Q000737:chemistry*; D006835:Hydrazones / Q000138:chemical synthesis* / Q000737:chemistry*; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D006835:Hydrazones; C585708:N-propargylic sulfonylhydrazone; D011720:Pyrazoles; D011799:Quinazolines; D006046:Gold