专利号:US-9102698-B2 优先权日:2007-03-14 标 题:Process for the synthesis of IB-MECA 发明人:BRUZINSKI PAUL; LIU XUEJUN; GIBB CAMERON; HERNANDEZ-ABAD PEDRO E 权利人:BRUZINSKI PAUL; LIU XUEJUN; GIBB CAMERON; HERNANDEZ-ABAD PEDRO E; CAN FITE BIOPHARMA LTD 摘要:The present disclosure provides a method for the synthesis of IB-MECA. More specifically, the present disclosure provides a simple and high yield method for Good Manufacturing Production (GMP) of IB-MECA. The method involves the reaction of 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine; reaction of the diol protected 6-halopurine with a nucleophile (e.g. methylamine); substitution of the halogen group with iodobenzylamine and removal of the diol protecting group.
专利号:US-8076499-B2 优先权日:2009-08-13 标 题 :Method for preparing precursor of radioactive 3-iodobenzylguanidine 发明人:LIU SHOW-WEN; LIN CHENG-HSIEN; LIN TSYH-LANG; HSU CHENG-FANG 权利人:LIU SHOW-WEN; LIN CHENG-HSIEN; LIN TSYH-LANG; HSU CHENG-FANG; ATOMIC ENERGY COUNCIL 摘要:A method for preparing a precursor of radioactive 3-iodobenzylguanidine- N,N′-bis(tert-butyloxycarbonyl)-3-(tri-n-butyltin)benzylguanidine) (MSnBG) is revealed. The method includes following steps. Firstly, obtain 3-iodobenzylguanidine bicarbonate by an addition reaction between 3-iodobenzylamine hydrochloride and cyanamide. Use di-tert-butyl dicarbonate as a protecting agent for NH group and convert 3-iodobenzylguanidine bicarbonate into N,N′-bis(tert-butyloxycarbonyl)-N-(3-iodobenzyl) guanidine. At last, under catalysis of bis(triphenylphosphine) palladium dichloride, obtain a final product MSnBG by a substitution reaction between N,N′-bis(tert-butyloxycarbonyl)-N-(3-iodobenzyl) guanidine and bis(tri-n-butyltin). MSnBG is used in no-carrier-added synthesis of [*l]MIBG.
专利号:US-5565185-A 优先权日:1994-07-20 标 题 :Process for the preparation of radiolabeled meta-halobenzylguanidine 发明人:HUNTER DUNCAN H; GOEL ALOK; FLANAGAN RICHARD J 权利人:MERCK FROSST CANADA INC 摘要:The present invention provides a no-carrier-added synthesis of radiolabeled meta-halobenzylguanidine by halodestannylation which comprises reacting a meta-trialkylstannylbenzylguanidine with a source of radionuclide of a halogen. The present invention also provides meta-trialkylstannylbenzylguanidine as intermediates in the afore-mentioned process.
专利号:US-2010087636-A1 优先权日:2007-03-14 标题:Process for the synthesis of ib-meca
专利号:WO-2008111082-A1 优先权日:2007-03-14 标题 :Process for the synthesis of ib-meca
专利号:DK-2137202-T3 优先权日:2007-03-14 标题:PROCEDURE FOR SYNTHESIS OF IB-MECA
参考标题:A Mild And General One-Pot Synthesis Of Densely Functionalized Diaryliodonium Salts 作者:Linlin Qin,Bao Hu,Kiel D. Neumann,Ethan J. Linstad,Katelyenn Mccauley,Jordan Veness,Jayson J. Kempinger,Stephen G. Dimagno |发布日期:2015.9 摘要:Diaryliodonium Salts Are Powerful And Widely Used Arylating Agents In Organic Chemistry. Here We Report A Scalable, Synthesis Of Densely Functionalized Diaryliodonium Salts From Aryl Iodides Under Mild Conditions. This Two-Step, One-Pot Process Has Remarkable Functional Group Tolerance, Is Compatible With Commonly Employed Acid-Labile Protective Group Strategies, Avoids Heavy Metal And Transition Metal
合成参考文献
参考文献:10.1007/s11094-020-02178-y 摘要:Kapustyan AV, Buryak AA, Boiko VM. Development and Validation of an Analytical Method for Meta-Iodobenzylguanidine Sulfate Radiolabeled with 127I and 131I. Pharmaceutical Chemistry Journal. 2020 May 16;54(2):201–7. doi: 10.1007/s11094-020-02178-y.