专利号:US-5786515-A 优先权日:1995-09-15 标题 :Synthesis of α-chloro or fluoro ketones 发明人:DOLLING ULF H; FREY LISA F; TILLYER RICHARD D; TSCHAEN DAVID M 权利人:MERCK & CO INC 摘要:A simple, high yielding synthesis of a-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-N-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.
专利号:WO-2024110994-A1 优先权日:2022-11-25 标题 :A process for the preparation of ledipasvir 发明人:GANGARAJULA SUDHAKAR; CHENNAM RAMU; KUMARAGURU THENKRISHNAN; BABURAO RODE HARIDAS; MADDI REDDY SRIDHAR; CHADA REDDY RAJI; GHOSH SUBHASH 权利人:COUNCIL OF SCIENT AND INDUSTRIAL RESEARCH AN INDIAN REGISTERED BODY INCORPORATED UNDER THE REGN OF S 摘要:The present disclosure relates to process for the preparation of Ledipasvir (I) or of its pharmaceutically acceptable salts. The present disclosure also provides novel intermediates (IV–XI) that are used in the synthesis of Ledipasvir. The main strategies of the present invention are late-stage functionalization such as difluorination and cyclopropanation of the key intermediates of Ledipasvir (I). (Formula (I))
专利号:US-2024309003-A1 优先权日:2021-05-04 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN; PANDYA BHAUMIK; KAPLAN ALAN 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-9718807-B2 优先权日:2012-06-05 标 题 :Synthesis of antiviral compound 发明人:SCOTT ROBERT WILLIAM; VITALE JUSTIN PHILIP; MATTHEWS KENNETH STANLEY; TERESK MARTIN GERALD; FORMELLA ALEXANDRA; EVANS JARED WAYNE 权利人:GILEAD PHARMASSET LLC 摘要:The present disclosure provides processes for the preparation of a compound of formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.
专利号:US-9527877-B2 优先权日:2012-06-29 标题 :Metal complexes, their application and methods of carrying out of metathesis reaction 发明人:SKOWERSKI KRZYSZTOF; BIENIEK MICHAL 权利人:APEIRON SYNTHESIS SA 摘要:This disclosure relates to new metal complexes, such as compounds of Formula 1, and their application in olefin or alkyne metathesis and to methods of carrying out olefin metathesis reactions.
专利号:US-2018351104-A1 优先权日:2012-11-02 标 题:3-substituted tellurophenes and related compounds 发明人:SEFEROS DWIGHT; JAHNKE ASHLEE 权利人:GOVERNING COUNCIL UNIV TORONTO 摘要:Monomeric 3-substituted tellurophene compounds, as well as their use in the synthesis of oligomeric and/or polymeric compounds consisting of two or more tellurophene-2,5-diyl groups which are covalently linked to each other are disclosed, as is the use of said oligomers and polymers in devices such as diodes and solar cells, electrodes and semiconductors.
[参考文献]: James T Hodgkinson, Et Al. Microwave And Flow Syntheses Of Pseudomonas Quinolone Signal (Pqs) And Analogues. Org Biomol Chem. 2011 Jan 7;9(1):57-61.
合成参考文献
摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2015). 摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2019) 摘要:Ptzel, M.; Pritz, S.; Liebscher, J., Science of Synthesis, (2005) 21, 486. 摘要:Lipton, M. F.; Mauragis, M. A., Science of Synthesis, (2005) 21, 540.