title: Leonurine, an improved synthesis.
abstract: Leonurine (1) is the uterotonic principle of Leonurus artemisia. We have developed a simple, high-yield synthetic procedure of 1 that is adaptable to large scale preparation. The synthesis involves the condensation of syringic acid and 4-guanidino-1-butanol hydrochloride in the presence of DDC using 1:1 HMPT-ether as solvent. The synthetic leonurine showed uterotonic activity in vivo and in vitro.
mesh_terms: D000818:Animals; D005260:Female; D005707:Gallic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D006146:Guanidines / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D008722:Methods; D051381:Rats; D014590:Uterine Contraction / Q000187:drug effects*
chemical_list: D006146:Guanidines; D005707:Gallic Acid