BZA-[99mTcN], [99mTcN]-BZA

Chemical Name: [4-[4-[N-[2-(Diethylamino)ethyl]carbamoyl]benzyl]-2,6,6,9-tetramethyl-4,7-diazadecane-2,9-dithiol]nitrilotechnecium
项目整合开发状态: Preclinical
项目研究机构: CIS Bio International (Originator), INSERM (Originator)
合成路线:The cyclization of 2,2,5,5-tetramethyl-3,4-dithiahexane-1,6-dial (I) with 2-methylpropane-1,2-diamine (II) in hoot ethanol gives 3,3,6,6,10,10-hexamethyl-1,2-dithia-5,8-diazacyclodeca-4,8-diene (III),which is reduced with NaBH3CN in ethanol to afford the corresponding cyclodecane compound (IV).The condensation of (IV) with 4-(bromomethyl)benzoic acid methyl ester (V) by means of K2CO3 in refluxing acetonitrile yields the adduct (VI),which is condensed with 2-(diethylamino)ethylamine (VII) by means of Al(CH3)3 in refluxing dichloromethane to provide the corresponding amide (VIII).Ring opening of (VIII) at the S-S bond by means of dithiothreitol (DTT) and TEA in MeOH gives the dithiol (IX),which is finally treated with TcO4Na,SnCl2 and NaOH in ethanol/water.

合成路线:The cyclization of 2,2,5,5-tetramethyl-3,4-dithiahexane-1,6-dial (I) with 2-methylpropane-1,2-diamine (II) in hot ethanol gives 3,3,6,6,10,10-hexamethyl-1,2-dithia-5,8-diazacyclodeca-4,8-diene (III),which is reduced with NaBH3CN in ethanol to afford the corresponding cyclodecane compound (IV).The condensation of (IV) with 4-(bromomethyl)benzoic acid methyl ester (V) by means of K2CO3 in refluxing acetonitrile yields the adduct (VI),which is condensed with 2-(diethylamino)ethylamine (VII) by means of Al(CH3)3 in refluxing dichloromethane to provide the corresponding amide (VIII).Ring opening of (VIII) at the S-S bond by means of dithiothreitol (DTT) and TEA in methanol gives the dithiol (IX),which is finally treated with TcO4Na,PPh3 and N,S-dimethyldithiocarbazate (MDTCZ) in ethanol / 1M HCl.