专利号:US-2024018099-A1 优先权日:2020-11-19 标题 :Synthesis of prostate specific membrane antigen (psma) ligands 发明人:ANDREAE FRITZ 权利人:NOVARTIS AG 摘要:The present disclosure relates to the synthesis of prostate specific membrane antigen (PSMA) ligands that are useful in the treatment of diseases like cancer. In particular, the disclosure relates to a method for synthesizing PSMA ligands having a glutamate-urea-lysine (GUL) moiety and a chelating agent that can comprise a radiometal.
专利号:US-10815194-B2 优先权日:2016-11-14 标题 :Process for the preparation of mono-protected α,ω-diamino alkanes 发明人:MENGE WIRO MICHAEL PETRUS BERNARDUS 权利人:BYONDIS BV 摘要:The present invention relates to a process for the synthesis of mono-protected α,ω-diamino alkanes, the use of said process in a process for the synthesis of a linker drug comprising an α,ω-diamino alkane moiety and the use of the process of the present invention in a process for preparing an antibody-drug conjugate comprising an α,ω-diamino alkane moiety.
专利号:US-9428524-B2 优先权日:2010-05-25 标 题:Synthetic process for the manufacture of ecteinascidin compounds 发明人:MARTIN LÓPEZ MA JESÚS; FRANCESCH SOLLOSO ANDRÉS; CUEVAS MARCHANTE MARIA DEL CARMEN 权利人:MARTIN LÓPEZ MA JESÚS; FRANCESCH SOLLOSO ANDRÉS; CUEVAS MARCHANTE MARIA DEL CARMEN; PHARMA MAR SA 摘要:This invention relates to compounds of formula II: wherein R 1 , R 2 , Prot SH , and Prot NH are as defined, to processes for the synthesis of ecteinascidins of formula I from compounds of formula II, and to processes for the synthesis of compounds of formula II.
专利号:WO-2014108526-A1 优先权日:2013-01-11 标题 :Synthetic process for the manufacture of pipecolidepsin compounds 发明人:PELAY GIMENO MARTA; GARCÃ?A-RAMOS YESICA; TULLA PUCHE JUDIT; ALBERICIO PALOMERA FERNANDO; MARTÃ?N LÓPEZ M JES S 权利人:PHARMA MAR SA 摘要:(I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , n and Y are as described. The invention provides a process for the synthesis of complex pipecolidepsin and related compounds of formula (I), opening a new field of compounds with useful biological properties. The invention also provides intermediates, useful in the synthesis of compounds of formula (I).
专利号:US-8138272-B2 优先权日:2006-05-22 标 题:Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds 发明人:KONRADI ANDREI W; SMITH JENIFER L 权利人:KONRADI ANDREI W; SMITH JENIFER L; ELAN PHARM INC 摘要:This invention provides an improved synthesis of polymer conjugates of formula (I), n nof agricultural, therapeutic, and food additive compounds. In particular, a process is described for the preparation of conjugates by treating primary or secondary alcohol substituents of active compounds with polymeric nucleophiles using “Mitsunobuâ€? or related reaction conditions.
专利号:US-9035070-B2 优先权日:2010-07-30 标 题 :Process for the preparation of 1-aryl-pyrazol-3-one intermediates useful in the synthesis of sigma receptors inhibitors 发明人:BARTRA SANMARTI MARTÃ?; BERENGUER MAIMO RAMON; MEDRANO RUPEREZ JORGE; GARCIA GOMEZ JORGE; ARIZA PIQUER JAVIER 权利人:BARTRA SANMARTI MARTÃ?; BERENGUER MAIMO RAMON; MEDRANO RUPEREZ JORGE; GARCIA GOMEZ JORGE; ARIZA PIQUER JAVIER; ESTEVE QUÃ?MICA S A 摘要:The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.
[参考文献]: Miguel A. Bailén, Et Al. 2-Mercaptopyridone 1-Oxide-Based Uronium Salts: New Peptide Coupling Reagents(1)(,)(2). J Org Chem. 1999 Nov 26;64(24):8936-8939.
合成参考文献
参考文献:10.1093/jof/39.10.880 摘要:. Correspondence. 1941 Oct 01;39(10):880–91. doi: 10.1093/jof/39.10.880.