专利号:US-6723798-B1 优先权日:2000-08-28 标 题:Resins having vinyl ether linker for the solid phase organic synthesis 发明人:YOO SUNGEUN; GONG YOUNGDAE; SEO JINSOO 权利人:KOREAN RES INST OF CHEMICAL TE 摘要:The present invention relates to a resin having a vinyl ether linker and more particularly, to a resin having a vinyl ether linker expressed by formula (I), useful for the synthesis of compounds having hetero atoms such as alcohol, thiol, imidazole, triazole and tetrazole by employing combinatorial chemical synthesis on solid supports.
专利号:US-2023303474-A1 优先权日:2020-07-30 标 题 :Total syntheses of specialized pro-resolving mediators (spms), structural isomers and structural analogs 发明人:MARETTE ANDRÉ; MALTAIS RENÉ; POIRIER DONALD; SANCÉAU JEAN-YVES 权利人:UNIV LAVAL 摘要:A method for the synthesis of specialized pro-resolving mediators, structural isomers thereof and analogs thereof is disclosed herein. The method comprises reacting a compound of the formula (I): n n n n n n n n n n n n wherein R 1 is alkyl (C≤12) , cycloalkyl (C≤12) , alkenyl (C≤12) , alkylidene (C≤12) , alkynyl (C≤12) , aryl, aralkyl, heteroaryl or heteroaralkyl; and X 1 , X 2 and X 3 are each independently hydroxy or OP, wherein P is a hydroxy protecting or hydroxy activating group; with a reducing agent under conditions sufficient to produce a compound of the formula (II): n n n n n n n n n n n n n n n n wherein: R 1 , X 1 , X 2 and X 3 are as defined above. n n n n n Novel protectins, more specifically novel structural isomers and analogs of PD1 and PDX are also disclosed.
专利号:US-10807953-B2 优先权日:2015-03-02 标题:Processes and intermediates for the preparation of Pimavanserin 发明人:BILJAN TOMISLAV; DOGAN JASNA; METSGER LEONID; PIPERCIC SARA MORASI; RATKAJ MARINA; SKUGOR MAJA MATANOVIC; WANG YI 权利人:PLIVA HRVATSKA D O O 摘要:The present disclosure relates to novel, safe and efficient processes for the synthesis of Pimavanserin and salts thereof, as well as novel intermediates that can be used in these processes.
专利号:US-6933303-B2 优先权日:2001-10-19 标 题:Heteroaryl-fused nitrogen heterocycles as therapeutic agents 发明人:MJALLI ADNAN M M; ANDREWS ROBERT C; XIE RONGYUAN; YARRAGUNTA RAVINDRA R; REN TAN 权利人:TRANSTECH PHARMA INC 摘要:This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases, the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.
专利号:CN-112028900-A 优先权日:2020-09-10 标 题:Synthesis of Star-shaped Polymers and Unimolecular Micelles by Photo-Controlled In-situ Bromine-Iodine Conversion RDRP Method
专利号:US-5521179-A 优先权日:1991-04-18 标题 :Heterocyclic amides 发明人:BERNSTEIN PETER R; SHAW ANDREW; THOMAS ROYSTON M; WARNER PETER; WOLANIN DONALD J 权利人:ZENECA LTD 摘要:The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.
[参考文献]: Rong-Qing Mei, Et Al. A New Phenol Derivative Isolated From Mangrove-Derived Fungus Eupenicillium Sp. Hj002. Nat Prod Res. 2020 Jan 21;1-7. [参考文献]: S H Jung, Et Al. Enantioselective Preparation Of Metoprolol And Its Major Metabolites. Arch Pharm Res. 2000 Jun;23(3):226-9.
合成参考文献
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 396. 摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198 摘要:Angelini, E.; Sarlah, D., Science of Synthesis: Dearomatizations, (2026) . 摘要:Angelini, E.; Sarlah, D., Science of Synthesis: Dearomatizations, (2026) . 参考文献:10.1038/nchem.1506 摘要:Over B, Wetzel S, Grütter C, Nakai Y, Renner S, Rauh D, Waldmann H. Natural-product-derived fragments for fragment-based ligand discovery. Nat Chem. 2013 Jan;5(1):21–8. doi: 10.1038/nchem.1506.