我们已经开发了一种新的催化方法,用于通过PdPt-Fe 3 O 4纳米颗粒(NP)催化剂通过芳基腈与硝基烷烃的还原胺化反应,实现不对称仲胺的一锅级联反应。与单金属Pd–Fe 3 O 4或Pt–Fe 3 O 4相比,双金属催化剂的使用提高了反应性和选择性。NP催化剂。使用这种双金属催化体系,我们成功地在温和条件下合成了各种不对称仲胺。然而,含有给电子取代基的芳基腈相当耐还原胺化,当使用六氟异丙醇(HFIP)作为助溶剂时,不对称仲胺的反应选择性和收率大大提高。使用催化剂体系,可以由2-硝基苯基乙腈一锅克级地合成吲哚。由于Fe 3 O 4载体的磁性,双金属催化剂可以容易地使用外部磁体至少循环四次。
NARGENICIN COMPOUNDS AND USES THEREOF AS ANTIBACTERIAL AGENTS
申请人:Merck Sharp & Dohme Corp.
公开号:US20180186808A1
公开(公告)日:2018-07-05
The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against
Mycobacterium tuberculosis
. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by
Mycobacterium tuberculosis
by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.