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Synthesis of an Azabicyclo[3.1.0]hexanone-Containing Inhibitor of NF-κΒ Inducing Kinase via Catalytic C–H Activation
Synthesis ( IF 2.2 ) Pub Date : 2020-09-15 , DOI: 10.1055/s-0040-1707279
James J. Crawford 1 , Daohong Liao 2 , Aleksandr Kolesnikov 1 , Wendy Lee 1 , Matthew L. Landry 1
Affiliation  


Abstract

The synthesis of an azabicyclo[3.1.0]hexanone-containing inhibitor of the nuclear factor-κB inducing kinase (NIK) is reported. The initial route to this compound was streamlined from 13 to 7 linear steps through the use of a catalytic, enantioselective C–H activation step. A procedure for lactam oxidation was identified that avoided use of peroxides on scale. These synthetic improvements allowed for the synthesis of multigram quantities of the desired NIK inhibitor for in vivo profiling.



Publication History

Received: 28 July 2020

Accepted: 12 August 2020

Publication Date:
15 September 2020 (online)

© 2020. Thieme. All rights reserved

Georg Thieme Verlag KG
Rüdigerstraße 14, 70469 Stuttgart, Germany



中文翻译:

催化CH活化合成含氮杂双环[3.1.0]己酮的NF-κof诱导激酶抑制剂


摘要

据报道合成了含氮杂双环[3.1.0]己酮的核因子-κB诱导激酶(NIK)抑制剂。通过使用催化,对映选择性的CH活化步骤,使该化合物的起始路线从13个线性步骤简化为7个线性步骤。内酰胺氧化的程序已确定可避免大规模使用过氧化物。这些合成的改进使得可以合成多克数量的所需NIK抑制剂用于体内分析。



出版历史

收到:2020年7月28日

接受:2020年8月12日

发布日期:
2020年9月15日(在线)

©2020年。Thieme。版权所有

Georg Thieme Verlag
KGRüdigerstraße14,70469斯图加特,德国

更新日期:2020-09-16
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