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Mn- and Co-Catalyzed Aminocyclizations of Unsaturated Hydrazones Providing a Broad Range of Functionalized Pyrazolines
JACS Au Pub Date : 2021-06-11 , DOI: 10.1021/jacsau.1c00176
Moritz Balkenhohl 1 , Sebastian Kölbl 1 , Tony Georgiev 1 , Erick M Carreira 1
Affiliation  

Manganese- and cobalt-catalyzed aminocyclization reactions of unsaturated hydrazones are reported. Whereas manganese catalysis provides access to pyrazoline and tetrahydropyridazine alcohols, cobalt catalysis for the first time paves the way for the selective formation of pyrazoline aldehydes. Furthermore, various functional groups including hydroperoxide, thiol derivatives, iodide, and bicyclopentane may be introduced via manganese-catalyzed ring-forming aminofunctionalization. A progesterone receptor antagonist was prepared using the aminocyclization protocol.

中文翻译:

锰和共催化的不饱和腙的氨基环化提供了广泛的官能化吡唑啉

报道了不饱和腙的锰和钴催化的氨基环化反应。锰催化提供了获得吡唑啉和四氢哒嗪醇的途径,而钴催化首次为选择性形成吡唑啉醛铺平了道路。此外,可以通过锰催化的成环氨基官能化引入各种官能团,包括氢过氧化物、硫醇衍生物、碘化物和双环戊烷。使用氨基环化方案制备孕酮受体拮抗剂。
更新日期:2021-07-26
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