A concise and enantioselective synthesis of novel HIV-1 protease transition state mimics

✍ Scribed by Bruce D. Dorsey; Kevin J. Plzak; Richard G. Ball

• Book ID: 104224975
• Publisher: Elsevier Science
• Year: 1993
• Tongue: French
• Weight: 286 KB
• Volume: 34
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/s0040-4039(00)91945-2

✦ Synopsis

Novel HIV-1 protease inhibitors have been prepared in a enantioselective manner via an Evans asymmetric aldol, Claisen rearrangement and icdolactonization. X-ray crystallographic analysis was used to confirm the absolute configuration of the newly created stereogenic centers.

The alarming spread of human immunodeficiency virus type 1 (HIV-l), the etiologic agent of the acquired immunodeficiency syndrome (AIDS),1 has initiated an urgent quest to comprehend and control this disease. This has led to the discovery of a virally encoded homodimeric aspartyl protease, which is responsible for processing the gag and pof gene products that allow for the organization of core structural proteins.