-药物合成数据库

【药物名称】

化学结构式(Chemical Structure):

参考文献No.	57248
标题:	Aminoderivs. of biotin and their conjugates with macrocyclic chelating agents
作者:	Paganelli, G.; Chinol, M.; Ginanneschi, M. (Sigma-Tau Industrie Farmaceutiche Riunite SpA)
来源:	WO 0266075

合成路线图解说明: The coupling of biotin (I) with N-Boc-1,6-diaminohexane (II) by means of HATU yields the amide (III). Subsequent acidic cleavage of the N-Boc protecting group of (III) gives the amine (IV), which is reduced by borane in THF to furnish the diamine (V). Finally, coupling of (V) with the tetra-aza macrocyclic ligand (VI), followed by radiolabeling with 90Y, affords the target compound. (1,2)

参考文献No.	737849
标题:	A new biotin derivative-DOTA conjugate as a candidate for pretargeted diagnosis and therapy of tumors
作者:	Sabatino, G.; Chinol, M.; Paganelli, G.; Papi, S.; Chelli, M.; Leone, G.; Papini, A.M.; De Luca, A.; Ginanneschi, M.
来源:	J Med Chem 2003,46(14),3170

合成路线图解说明: The coupling of biotin (I) with N-Boc-1,6-diaminohexane (II) by means of HATU yields the amide (III). Subsequent acidic cleavage of the N-Boc protecting group of (III) gives the amine (IV), which is reduced by borane in THF to furnish the diamine (V). Finally, coupling of (V) with the tetra-aza macrocyclic ligand (VI), followed by radiolabeling with 90Y, affords the target compound. (1,2)