Efficient synthesis of unsymmetrical 1,4-disubstituted-2,3-diketopiperazines via tandem reductive amination–cyclization

✍ Scribed by Douglas C Beshore; Christopher J Dinsmore

• Book ID: 104211114
• Publisher: Elsevier Science
• Year: 2000
• Tongue: French
• Weight: 123 KB
• Volume: 41
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/s0040-4039(00)01565-3

✦ Synopsis

Herein we report the efficient syntheses of 1,4-disubstituted-2,3-diketopiperazines and 1,4,5-trisubstituted-2,3-diketopiperazines, which feature a tandem reductive amination and acylation. Aliphatic and aromatic primary amines serve as viable nucleophiles under the mild reaction conditions.