Leonurine, an improved synthesis

Article abstract of DOI:10.1007/BF01960323

The uterotonic principle of Leonurus artemisia, a plant leaf, is leonurine. This paper reports the development of a simple, high-yield synthetic procedure of reproducing leonurine that is adaptable to large-scale preparation. The synthetic process includes condensation of syringic acid and 4-guanidino-1-butanol hydrochloride in the presence of dicyclohexylcarbodiimide, using 1:1 hexamethylphosphoric triamide-ethyl ether as solvent. Synthetic leonourine showed uterotonic activity in vitro and in vivo, just like its naturally occurring counterpart.