专利号:WO-2012003598-A1 优先权日:2010-07-06 标 题 :Intermediates for the synthesis of 1,2-bis(4,7-dimethyl-1,4,7-triazacyclonon-1-yl)-ethane and preparation method thereof 发明人:HAGE RONALD; KOEK JEAN HYPOLITES; RUSSELL STEPHEN WILLIAM; WANG XIAOHONG; WOLF LODEWIJK VAN DER; ZHANG JIANRONG; ZHAO WEI 权利人:UNILEVER PLC; UNILEVER NV; UNILEVER HINDUSTAN; HAGE RONALD; KOEK JEAN HYPOLITES; RUSSELL STEPHEN WILLIAM; WANG XIAOHONG; WOLF LODEWIJK VAN DER; ZHANG JIANRONG; ZHAO WEI 摘要:The present invention provides intermediates for the synthesis of 1,2-bis(4,7-dimethyl-1,4,7-triazacyclonon-1-yl)-ethane and preparation method thereof. The intermediates are protonated salts of 1,4-ditosylate-1,4,7-triazacyclononane or 1,4-dibenzenesulphonate-1,4,7-triazacyclononane. The preparation method of 1,4-diarylsulfonate-1,4,7-triazacyclononane (compound A) comprises reacting 1,4,7-triarylsulfonate-1,4,7-triazacyclononane (compound B) in an acidic medium comprising sulphuric acid, wherein the molar ratio of B to sulphuric acid is in the range from 1 : 0.5 to 1 : 10, or reacting 1,4,7-triarylsulfonate-1,4,7-triazacyclononane (compound B) in an acidic medium and working up the acidic medium when the conversion of B to A is at least 50 mol % yielding compound A.
专利号:US-8907082-B2 优先权日:2010-07-06 标 题 :1,2-bis-(4,7-dimethyl-1,4,7-triazacyclonon-1-yl)-ethane and intermediate for the synthesis of same 发明人:HAGE RONALD; KOEK JEAN HYPOLITES; RUSSELL STEPHEN WILLIAM; VAN DER WOLF LODEWIJK; ZHANG JIANRONG; ZHAO WEI; WANG XIAOHONG 权利人:HAGE RONALD; KOEK JEAN HYPOLITES; RUSSELL STEPHEN WILLIAM; VAN DER WOLF LODEWIJK; ZHANG JIANRONG; ZHAO WEI; WANG XIAOHONG; CATEXEL LTD 摘要:The present invention provides improved processes for the synthesis of 1,4-ditosyl-1,4,7-triazacyclonone, comprising deprotecting a compound of formula (C): n nwherein P is tosylate or arylsulfonate, with an acidic medium to form 1,2-bis(1,4,7-triazacyclonon-1-yl)-ethane; and subsequently adding formaldehyde and formic acid to the acidic medium to form 1,2-bis-(4,7-dimethyl-1,4,7-triazacyclonon-1-yl)-ethane (Me 4 -DTNE). The syntheses of intermediates are also disclosed.
专利号:US-9988388-B2 优先权日:2012-11-21 标 题:Synthesis of imidazo[1,2-a]pyrazin-4-ium salts for the synthesis of 1,4,7-triazacyclononane (tacn) and N- and/or C- functionalized derivatives thereof 发明人:DENAT FRANCK; DESOGERE PAULINE; BERNHARD CLAIRE; ROUSSELIN YOANN; BOSCHETTI FREDERIC 权利人:UNIV BOURGOGNE; CENTRE NAT RECH SCIENT 摘要:A compound with formula (V′) n nthe synthesis method for compound (V′), and its use for the preparation of 1,4,7-triazacyclononane (tacn) and N- and/or C-functionalized derivatives thereof, particularly compounds with formula (I)n n nAlso, metallic complexes comprising a ligand with formula (I) and a metal and their use for imaging.
专利号:WO-2025088147-A1 优先权日:2023-10-27 标题 :Theranostic psma-targeting ligands for the diagnosis and treatment of psma-expressing cancers and their solid phase synthesis 发明人:Schäfer Martin; BAUDER-WUEST ULRIKE; ROSCHER MAREIKE; REMDE YVONNE; BENEÅ OVà -SCHÄFER MARTINA; BARINKA CYRIL; KUTILOVà ZSÓFIA; MOTLOVà LUCIA 权利人:DEUTSCHES KREBSFORSCHUNGSZENTRUM STIFTUNG DES OEFFENTLICHEN RECHTS 摘要:The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and radiopharmaceuticals for the treatment of various disease states of PSMA-expressing cancers, especially prostate cancer, and metastases thereof. Further the present invention provides synthetic procedures for the synthesis of such PSMA-targeting ligands.
专利号:US-2025049714-A1 优先权日:2021-12-09 标题 :Synthesis of ester, carbonate, and carbamate-derived novel biodegradable ionizable lipids from methyl ricinoleate or methyl 12-hydroxystearate and its applications 发明人:ANDERSON DANIEL GRIFFITH; RHYM LUKE HYUNSIK; LI BOWEN; GORDON AKIVA; RAJITH SINGH MANAN; WITTEN JACOB 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Provided herein are compounds, such as compounds of Formula (I), and pharmaceutically acceptable salts, hydrates, solvates, polymorphs, co-crystals, tautomers, stereoisomers, and isotopically labeled derivatives thereof, and compositions, methods, uses, and kits thereof. The compounds provided herein are lipids useful for delivery of polynucleotides, such as mRNA, for the treatment and/or prevention of various diseases and conditions (e.g., genetic disease, proliferative disease, hematological disease, neurological disease, liver disease, spleen disease, lung disease, painful condition, psychiatric disorder, musculoskeletal disease, a metabolic disorder, inflammatory disease, or autoimmune disease).
专利号:US-2025313580-A1 优先权日:2022-05-19 标题 :Synthesis of fluorosilyl compounds 发明人:FORD THONAN LEE; THOMAS ALEXANDER JAMES FLOY; RAHMAN SABITUR 权利人:BLUE EARTH THERAPEUTICS LTD 摘要:The disclosures herein relate to methods of synthesising a compound of formula (1): n n n n n n n n n n wherein PG, R 2 and R 3 are as defined herein, and the use of said methods in the manufacture of conjugates that bind to PSMA.
[参考文献]: Guo Jf, Et, Al. Trans-[参考文献]: Nonat A, Et, Al. Structural And Photophysical Studies Of Highly Stable Lanthanide Complexes Of Tripodal 8-Hydroxyquinolinate Ligands Based On 1,4,7-Triazacyclononane. Inorg Chem. 2009 May 4;48(9):4207-18.
合成参考文献
参考文献:10.1021/ol010256p|10.1021/ol016291d 摘要:Warden A, Graham B, Hearn MT, Spiccia L. Synthesis of novel derivatives of 1,4,7-triazacyclononane. Org Lett. 2001 Sep 06;3(18):2855–8. doi: 10.1021/ol016291d. 参考文献:10.1002/chem.200501390 摘要:Nonat A, Gateau C, Fries PH, Mazzanti M. Lanthanide complexes of a picolinate ligand derived from 1,4,7-triazacyclononane with potential application in magnetic resonance imaging and time-resolved luminescence imaging. Chemistry. 2006 Sep 18;12(27):7133–50. doi: 10.1002/chem.200501390. 参考文献:10.1007/s10787-007-0018-5 摘要:Tiekink ER. Anti-cancer potential of gold complexes. Inflammopharmacology. 2008 Jun;16(3):138–42. doi: 10.1007/s10787-007-0018-5.