A General Procedure for Synthesis of NG-Alkyl, and NG-Aryl-L-Arginines as Potential Nitric Oxide Synthase Inhibitors

Article abstract of DOI:10.1002/jccs.199800083

A general procedure for the synthesis of N^G-alkyl, and N^G-aryl-L-arginines with relatively high overall yield is reported. The key step involved the coupling of protected L-ornithine 4 with isothiourea 7 to give the fully protected N^G-aryl-L-arginine derivative 8. Subsequent deprotection of 8 in acidic condition provided the final target compound 9 with an overall yield of more than 80%.