Preparation Of ^99mTc-M₄ IDP And ^99mTc(CO)₃ -NSP-PA

Preparation of two radiolabeled compounds labeled with ^99mTc was described in this article.One was 1-Hydroxy-2- ( 4-methyl -1H-imidazoleyl ) -ethylidene-1,1-bisphosphonic(M4IDP) labeled with ^99mTc to afford ^99mTc-M4IDP. M4IDP was prepared by N-alkylation, ester hydrolation and phosphoric acid acylation from the raw material 4-methyl-1-H- imidazole. Then it was labeled by ^99mTc at the presence of reducing agent to afford ^99mTc-M4IDP. The labeling condition was optimized to the best condition: reaction time 30 minutes, pH 6, 100μg SnCl₂·2H₂O and 5 mg M4IDP. Under this condition, the labeling yield was more than 95%.The other was N-[2-propyloxy-4-(1-(2,2'-bipyridinemethyl)amino)acetylamino] phenylmethanesulfonamide(NSP-PA) labeled with ^99mTc(CO)₃ to afford ^99mTc(CO)3-NSP-PA. NSP-PA was prepared by hydroxyl-alkylation, amino-methylsulfonylation, nitro-reduction, amino-bromideacetylation and N-alkylation from the raw material 2-amino-5-nitrophenol. Then it was labeled with the freshly prepared ^99mTc(CO)₃ under appropriate conditions to gain target product ^99mTc(CO)₃-NSP-PA.M4IDP,NSP-PA and the intermediates were new compounds which were identified by Elemental Analysis,IR,MS and 1H-NMR.^99mTc-M4IDP and ^99mTc(CO)₃-NSP-PA were confirmed by HPLC and TLC. The results showed that both of the radiochemical puritys were over 90%. The product will be used in the further animal experiment.