81976-73-0Relevant academic research and scientific papers
Direct Palladium-Catalyzed β-Arylation of Lactams
Chen, Ming,Liu, Feipeng,Dong, Guangbin
, p. 3815 - 3819 (2018/03/13)
A direct and catalytic method is reported here for β-arylation of N-protected lactams with simple aryl iodides. The transformation is enabled by merging soft enolization of lactams, palladium-catalyzed desaturation, Ar?X bond activation, and aryl conjugate addition. The reaction is operated under mild reaction conditions, is scalable, and is chemoselective. Application of this method to concise syntheses of pharmaceutically relevant compounds is demonstrated.
Transition-Metal-Free Amine Oxidation: A Chemoselective Strategy for the Late-Stage Formation of Lactams
Griffiths, Robert J.,Burley, Glenn A.,Talbot, Eric P. A.
supporting information, p. 870 - 873 (2017/02/26)
A metal-free strategy for the formation of lactams via selective oxidation of cyclic secondary and tertiary amines is described. Molecular iodine facilitates both chemoselective and regioselective oxidation of C-H bonds directly adjacent to a cyclic amine. The mild conditions, functional group tolerance, and substrate scope are demonstrated using a suite of diverse small molecule cyclic amines, including clinically approved drug scaffolds.
TRICYCLIC DERIVATIVE
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Paragraph 0258; 0262, (2016/04/20)
Disclosed are compounds useful as inhibitors of phosphodiesterase 1 (PDE1), compositions thereof, and methods of using the same.
