专利号:US-11370736-B2 优先权日:2019-04-01 标 题:Synthesis of fluoro hemiacetals via transition metal-catalyzed fluoro ester and carboxamide hydrogenation 发明人:DUB PAVEL A; BATRICE RAMI J; GORDON JOHN C 权利人:TRIAD NAT SECURITY LLC 摘要:This application is directed to use of transition metal-ligand complexes to hydrogenate fluorinated esters and carboxamides into fluorinated hemiacetals. Methods for synthesis of certain ligands are also provided.
专利号:EP-2231627-B1 优先权日:2007-12-03 标题 :New process for the synthesis of moguisteine 发明人:VIGANO' ENRICO; ARRIGHI MASSIMILIANO; MOLTENI RENATO; LANFRANCONI SIMONA; LANDONIO ERNESTO 权利人:A M S A ANONIMA MATERIE SINT E AFFINI S P A 摘要:The invention relates to a process for the synthesis of moguisteine that is ethyl ester of (R,S)-3-[2-[(2-methoxyphenoxy)methyl]-1,3-thiazolidin-3-yl]-3-oxypropanoic acid which comprises the steps of forming a new cyclic intermediate of formula 2-[(2-methoxyphenoxy)methyl]-1,3-dioxolane (4), forming (R,S)-2-[(2-methoxyphenoxy)methyl]-1,3-thiazolidine (6) and reacting this latter with monoethylmalonic acid (7) or a salt thereof. The moguisteine of the invention is obtained in high yield and purity.
专利号:US-6448058-B1 优先权日:1997-09-12 标 题:Methods for solid phase synthesis of mercapto compounds and derivatives, combinatorial libraries thereof and compositions obtained thereby 发明人:PATEL DINESH V; NGU KHEHYONG; ZHOU JIANPING 权利人:VERSICOR INC 摘要:Methods of preparing combinatorial libraries of mercapto (thiol) compounds them and compositions obtained therefrom are disclosed. The compounds are synthesized on a solid support. Following synthesis, the compounds are optionally cleaved from the support. One such method of synthesis involves attack of an S-protected nucleophile on a resin functionalized with a leaving group. The invention also provides for screening the mercapto compounds for bioactive compounds; in particular, for inhibitors of MMPs.
专利号:US-9963472-B2 优先权日:2013-11-04 标 题 :Stable pantetheine derivatives for the treatment of pantothenate kinase associated neurodegeneration (PKAN) and methods for the synthesis of such compounds 发明人:JENKO BRANKO; KOSEC GREGOR; PETKOVIC HRVOJE; PODGORSEK BERKE AJDA; PAHOR JERCA; CUSAK ALEN; SIBON ODA CORNELIA MARIA; SRINIVASAN BALAJI 权利人:ACIES BIO D O O; UNIV GRONINGEN; ACADEMISCH ZIEKENHUIS GRONINGEN 摘要:The invention relates to (S)-acyl-4′-phosphopantetheine derivatives, methods of their synthesis, and related medical uses of such compounds. Preferred medical uses relate to the treatment of neurodegenerative diseases, such as PKAN.
专利号:WO-2025069039-A1 优先权日:2023-09-28 标题:An in situ process for the preparation of primary amine compounds 发明人:SAMANT RAJARAM; TONGRA MANOJ 权利人:SAMANT RAJARAM; TONGRA MANOJ 摘要:An in situ process for the preparation of primary amine compounds The invention disclosed herein relates to an in situ process for the preparation of primary amine compounds. Particularly, it relates to the preparation of primary amine compounds having general Formula (I). Formula (I) wherein n is 1 to 9 and X is -S, -N- or -O. More particularly, the present invention relates to the preparation of primary amine compounds with high yield and purity which is further used as potent intermediate in the synthesis of therapeutically active isothiocyanates (ITCs).
专利号:US-7393954-B2 优先权日:2002-12-12 标题:Process for the production of pentostatin aglycone and pentostatin 发明人:NADJI SOURENA; SMOOT JAMES; SAMPATH UMASHANKER 权利人:RELIABLE BIOPHARMACEUTICAL COR 摘要:A novel, scaleable and improved process for preparing pentostatin and its analogs is disclosed. The method comprises the diastereospecific synthesis of the nucleobase from commercially available L-Dialkyl tartarates.
摘要:C. J. Hawkins and D. D. Perrin. J. Chem. Soc. 1962, 1351. 参考文献:10.1186/1471-2105-9-263 摘要:Parravicini C, Ranghino G, Abbracchio MP, Fantucci P. GPR17: molecular modeling and dynamics studies of the 3-D structure and purinergic ligand binding features in comparison with P2Y receptors. BMC Bioinformatics. 2008 Jun 04;9():263.