Rapid assembly of 2-aminoimidazolones on solid support

✍ Scribed by Kexin Yang; Boliang Lou; Hossain Saneii

• Book ID: 104251246
• Publisher: Elsevier Science
• Year: 2002
• Tongue: French
• Weight: 173 KB
• Volume: 43
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/s0040-4039(02)00828-6

✦ Synopsis

A straightforward solid-phase synthesis of 2-aminoimidazolone derivatives is described. The synthesis starts with immobilization of thioureas onto solid support, followed by HBTU/DIEA assisted coupling of Boc-protected amino acids. Upon removal of the Boc group, intramolecular cyclization and simultaneous cleavage are promoted by polyamine resin to give the 2-aminoimidazolone derivatives in good yields and excellent purity.