THE USE OF METALLOCENIC ESTERS OF N-HYDROXYSUCCINIMIDE FOR METALLOHAPTEN SYNTHESIS

Different organometallic markers have been described in a new technique for the labelling of many drugs. Thus metallocenic esters of [GRAPHICAS] [M = (CO)3CrC6H5-; (CO)3CrC6H5-(CH2)3-; eta-C5H5-FeC5H4-; (CO)3Mn-eta-C5H4-; (CO)3Mn-eta-C5H4COCH2CH2-; eta-C5H4(eta-C5H5)Co+PF6-] react with primary or secondary amine drugs [DRUG-NHR] for a psychostimulant drug: amphetamine; tricyclic antidepressants-desipramine and nortriptyline; a vasodilator-histamine; an adrenergic substance-norfenefrine; and for a central stimulant-methamphetamine, to give the metallohaptens MCON(R)-DRUG. All these compounds have been fully characterized by different analytical methods and have potentialities for biological assays. This synthetic route was found better than one presented previously which utilized the metallocenic acid chloride MCOCI as intermediate, and could be proposed as a general synthetic route for labelling biological compounds which possess an amino group.