Many enzymes contain an essential arginyl residue at the active site. Butanedione and other simple a-diketones characteristically inactivate these enzymes by bonding covalently to arginine. l In an effort to confer specificity to this interaction, we have sought methods for incorporating an a-diketone moiety into polyfunctional inhibitors of such enzymes. 2 The ideal synthetic method for our purpose would involve the conversion of an existing ...
