新产品编号:946545
Chemical Name: [10-[N-[6-[5-[(3aS,4S,6aR)-2-Oxoperhydrothieno[3,4-d]imidazol-4-yl]pentylamino]hexyl]carbamoylmethyl]-1,4,7,10-tetraazacyclododecane-1,4,7-triacetato(3-)][90Y]yttrium(3+)
CAS No. 451478-45-8 (uncomplexed)
项目整合开发状态: Biological Testing
项目研究机构: Sigma-Tau (Originator)
合成路线: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)
📌 参考资料/链接：
参考文献标题:Aminoderivs.of biotin and their conjugates with macrocyclic chelating agents
文献作者:Paganelli,G.; Chinol,M.; Ginanneschi,M.(Sigma-Tau Industrie Farmaceutiche Riunite SpA)
参考来源:WO 0266075
📄 详细内容
合成路线: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)
参考文献标题:A new biotin derivative-DOTA conjugate as a candidate for pretargeted diagnosis and therapy of tumors
文献作者:Sabatino,G.; Chinol,M.; Paganelli,G.; Papi,S.; Chelli,M.; Leone,G.; Papini,A.M.; De Luca,A.; Ginanneschi,M.
参考来源:J Med Chem 2003,46(14),3170
产品链接: CAS No. 451478-45-8››