A one-pot preparation of N-2-mercaptobenzoyl-amino amides

TETRAHEDRON LETTERS

卷:52

Article

Bande, Robert J.¹  Appella, Daniel H.¹  Trenkle, William C.¹ 

[1] NIDDK, NIH, Bethesda, MD 20892 USA

关键词: HBTU;    Amide formation;    Thioester;    Topical microbicide;   

DOI  :  10.1016/j.tetlet.2011.05.115

来源: Elsevier

【 摘 要 】

The HIV-1 nucleocapsid (NCp7), structurally defined by zinc-binding domains, participates in crucial stages of the HIV-1 lifecycle and is mutationally nonpermissive, making it an attractive anti-HIV target. Mode of action studies have shown that the secondary structure and activity of NCp7 can be disrupted by acyl transfer from N-2-mercaptobenzoyl-amino amides. We have developed an improved one-pot reaction that affords N-2-mercaptobenzoyl-amino acids on multi-gram scales. This synthetic route allows for rapid modular construction and has greatly expanded the scope of easily accessible potential NCp7 inhibitors. Published by Elsevier Ltd.

【 授权许可】

Free