专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:WO-2021023634-A1 优先权日:2019-08-05 标 题 :PROCESS FOR THE SYNTHESIS OF PITOLISANT HCl 发明人:COLOMBANO GIAMPIERO; BARBERO MAURO; BOGOGNA LUIGI; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of pitolisant HCl of formula (I), from piperidine and 1-bromo-3-chloropropane. The process according to the invention is economically efficient and easily industrially scalable.
专利号:US-9777022-B2 优先权日:2012-10-02 标题 :Process for the preparation of macrocyclic polyazacarboxylate ligands and chelates 发明人:MOORE DENNIS A; RAJAGOPALAN RAGHAVAN 权利人:MALLINCKRODT LLC; GUERBET SA 摘要:The present disclosure relates generally to a process for the synthesis of 1,4,7,10-tetraazacyclododecane ligands, chelates, and derivatives thereof. In particular, the present disclosure is directed to a process for the synthesis of 1,4,7,10-tetraaza-1,4,7,10-tetrakis(carboxymethyl)cyclododecane (DOTA) ligands, corresponding DOTA-metal chelates, and various derivatives thereof.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-7807837-B2 优先权日:2004-05-07 标 题 :Scalable synthesis of imidazole derivatives 发明人:JONES TODD K; MANI NEELAKANDHA 权利人:JANSSEN PHARMACEUTICA NV 摘要:Imidazole derivatives, compositions containing them, methods of preparing them, including regioselective scale-up synthetic methods, and methods of using them.
专利号:US-2007021436-A1 优先权日:2005-06-10 标 题 :Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
[参考文献]: Shinya Harusawa, Et Al. Synthesis And Evaluation Of N-Alkyl-S-[3-(Piperidin-1-Yl)Propyl]Isothioureas: High Affinity And Human/rat Species-Selective Histamine H(3) Receptor Antagonists. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6415-20.
合成参考文献
摘要:Margaretha, P., Science of Synthesis Knowledge Updates, (2014) 2, 430.