发明名称 Methods for carbon isotope labeling synthesis by transition metal-promoted carbonylation via isocyanate using azides and carbon-isotope monoxide
摘要 Methods and reagents for transition metal-promoted carbonylation via isocyanate using carbon-isotope labeled carbon monoxide are provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.
申请公布号 US8741261(B2) 申请公布日期 2014.06.03
申请号 US20050086632 申请日期 2005.03.22
申请人 GE Healthcare Limited 发明人 Langstrom Bengt;Barletta Julien;Doi Hisashi;Suzuki Masaaki;Noyori Ryoji;Watanabe Yasuyoshi;Karimi Farhad
分类号 A61K51/00;A61M36/14;C07D345/00;C07D205/00;C07D213/46 主分类号 A61K51/00
代理机构 代理人
主权项 1. A method of using produced carbon-isotope enriched gas mixture in labeling synthesis, comprising: (a) providing a high pressure reaction chamber having a liquid inlet and a gas inlet in a bottom surface thereof, (b) providing an azide solution to be labeled comprising an azide of the formula R1—N3, wherein R1, is linear or cyclic lower alkyl or substituted alkyl, hydrogen, aryl or substituted aryl and optionally comprises carbonyl, hydroxy, thiol, halogen, nitrile, isonitrile, cyanate, isocyanate, thiocyanate, isothiocyanate functional groups, a transitional metal complex and a reagent, wherein the reagent is: R2, R3, R4, and R5 are independently linear or cyclic lower alkyl or substituted alkyl, hydrogen, aryl, or substituted aryl, and optionally comprise carbonyl, hydroxy, thiol, halogen, nitrile, isonitrile, cyanate, isocyanate, thiocyanate, isothiocyanate functional groups, (c) introducing a carbon-isotope monoxide enriched gas-mixture into the reaction chamber via the gas inlet, (d) introducing, at high pressure, said azide solution comprising said transition metal complex and one of said reagents into the reaction chamber via the liquid inlet, (e) waiting for a predetermined time while said labeling synthesis occurs, and (f) collecting the labeled compound from the reaction chamber, wherein the labeled compound is: wherein R1, is linear or cyclic lower alkyl or substituted alkyl, hydrogen, aryl or substituted aryl and optionally comprises carbonyl, hydroxy, thiol, halogen, nitrile, isonitrile, cyanate, isocyanate, thiocyanate, isothiocyanate functional groups and R2, R3, R4 and R5 are independently linear or cyclic lower alkyl or substituted alkyl, hydrogen, aryl or substituted aryl, and optionally comprise carbonyl, hydroxy, thiol, halogen, nitrile, isonitrile, cyanate, isocyanate, thiocyanate, isothiocyanate functional groups, and * is the labeled carbon position.
地址 Buckinghamshire GB