发明名称 Biotin stannane for HPLC-free radioiodination
摘要 The present teachings provide methods that enable the preparation and purification of radioiodinated vectors without the need for HPLC purification, as well as novel precursors which include biotin-like substituents useful in such methods.
申请公布号 US8927732(B2) 申请公布日期 2015.01.06
申请号 US201213435142 申请日期 2012.03.30
申请人 General Electric Company 发明人 Carter Randall Lee;Johnson Bruce Fletcher;Sood Anup;Rishel Michael James;Valliant John Fitzmaurice;Stephenson Karin Ann;Wu Tao;Yang Yang
分类号 C07F7/22;C07B59/00 主分类号 C07F7/22
代理机构 代理人 Gallagher Eileen B.
主权项 1. A method of preparing a radioiodinated compound, the method comprising: contacting a precursor with a radioactive iodide and an oxidant to form a reaction mixture comprising a radioiodinated compound, unreacted precursor, and reaction byproducts; and contacting the reaction mixture with avidin or streptavidin; thereby separating the radioiodinated compound from the precursor and the reaction byproducts; wherein the precursor is a compound of formula (I): or a pharmaceutically acceptable salt thereof; wherein:R1 is an aromatic or vinyl group capable of being substituted at an aromatic or vinylic carbon with iodide;R2 and R3 are each independently selected from R1; alkyl or alkoxyalkyl, each substituted with 0-4 R5 groups; or R2 and R3, along with the Sn atom to which they are attached, form a 3 to 8-membered ring that optionally includes one or more heteroatom selected from N, O, or S;Z is selected from —(C1-C4)alkylene-, —(C1-C4)alkylene-O—, arylene, heteroarylene, cycloalkylene or heterocycloalkylene, provided that m is at least 1 when Z is arylene or heteroarylene, and n=1 to 9, and provided that p=2-10 when Z is —(C1-C4)alkylene-O—;X is selected from —O— or —NR4—;R4 is selected from H or alkyl, wherein the alkyl is substituted with 0-4 R6 groups;each R5 is independently selected from —H, -halogen, —CN, —NO2, —NRaRb, —S(O)iRc, —C(═O)Rc, —C(═O)ORc, or —OC(═O)Rc;R6 is selected from —H, -halogen, —CN, —NO2, —NRaRb, —ORc, —S(O)iRc, —C(═O)Rc, —C(═O)ORc, or —OC(═O)Rc;Ra, Rb and Rc are each independently selected from —H or (C1-C6)alkyl;Y is selected from S, SO, SO2 or O;i is 0, 1, or 2; andm, n and p are each independently an integer from 0 to 10, wherein m+n+p≧1.
地址 Niskayuna NY US