专利号:US-10011580-B2 优先权日:2016-04-21 标题:Diastereoselective synthesis of (±)-epianastrephin, (±)-anastrephin and analogs thereof 发明人:WALSE SPENCER S; KUZMICH DANIEL 权利人:US AGRICULTURE 摘要:A process for the synthesis of trans-fused γ-lactones having Formula (IV) from substituted cyclic ketones having Formula (I). A diastereoselective synthesis of (±)-epianastrephin (1) (wherein: R 1 is ethenyl, R 2 and R 3 is methyl, and n is 1), (±)-anastrephin (2) (wherein: R 2 is ethenyl, R 1 and R 3 is methyl and n is 1), and analogs thereof (wherein: R 1 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 2 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 1 and R 2 together with the carbon atom they are attached form a C 3-6 cycloalkyl ring, R 3 is C 1-5 alkyl and n is 0-2):
专利号:US-6555686-B2 优先权日:2000-03-23 标题:Asymmetric synthesis of quinazolin-2-ones useful as HIV reverse transcriptase inhibitors 发明人:PARSONS RODNEY L; DOROW ROBERTA L; DAVULCU AKIN H; FORTUNAK JOSEPH M; HARRIS GREGORY D; KAUFFMAN GOSS S; NUGENT WILLIAM A; RADESCA LILIAN A 权利人:BRISTOL MYERS SQUIBB PHARMA 摘要:This invention relates generally to the asymmetric synthesis of quinazolin-2-ones that are useful as inhibitors of HIV reverse transcriptase. The synthesis is accomplished through the chiral ligand mediated addition of cyclopropylacetylide.
专利号:US-9884830-B2 优先权日:2004-05-21 标题 :Synthesis of tetracyclines and analogues thereof 发明人:MYERS ANDREW G; CHAREST MARK G; LERNER CHRISTIAN D; BRUBAKER JASON D; SIEGEL DIONICIO R 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.
专利号:US-12221452-B2 优先权日:2017-10-04 标题:Synthesis of cantharidin 发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R 权利人:VERRICA PHARMACEUTICALS INC 摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).
专利号:US-8486921-B2 优先权日:2006-04-07 标 题:Synthesis of tetracyclines and analogues thereof 发明人:MYERS ANDREW G; BRUBAKER JASON D; SUN CUIXIANG; WANG QIU 权利人:MYERS ANDREW G; BRUBAKER JASON D; SUN CUIXIANG; WANG QIU; HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetra-cycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals.
专利号:EP-4008687-A1 优先权日:2020-12-02 标 题:A method for the large scale synthesis of metal oxide nanosheets, and their uses 发明人:VINCENT MEWIN; ETACHERI VINODKUMAR 权利人:FUNDACION IMDEA MAT 摘要:The present invention relates to a rapid, scalable and inexpensive method for the synthesis of metal oxide nanosheets; the uses of the metal oxide nanosheets as electrode active materials and as catalyst; an electrode comprising the metal oxide nanosheets, a process for producing the electrode, a cell comprising the electrode and an energy storage and/or delivery system.
[参考文献]: Forrest S Gittleson, Et Al. Ultrathin Nanotube/nanowire Electrodes By Spin-Spray Layer-By-Layer Assembly: A Concept For Transparent Energy Storage. Acs Nano. 2015 Oct 27;9(10):10005-17. [参考文献]: Fumiya Urabe, Et Al. Total Synthesis Of (-)-Cinatrin C1 Based On An In(Otf)3-Catalyzed Conia-Ene Reaction. J Org Chem. 2013 Apr 19;78(8):3847-57. [参考文献]: Hua-Dong Xu, Et Al. One-Pot Protocol To Functionalized Benzopyrrolizidine Catalyzed Successively By Rh2(Oac)4 And Cu(Otf)2: A Transition Metal-Lewis Acid Catalysis Relay. Org Lett. 2015 Jan 2;17(1):66-9. [参考文献]: Krystyna Poreba, Et Al. The Synthesis Of 3,5,6,7-Tetrasubstituted Isoxazolo[参考文献]: Lihui Zhu, Et Al. In(Iii)/phco2H Binary Acid Catalyzed Tandem [2 + 2] Cycloaddition And Nazarov Reaction Between Alkynes And Acetals. Org Lett. 2013 Sep 6;15(17):4496-9.
合成参考文献
摘要:S100 | PFASREACH | List of PFAS identified in REACH 2019 | DOI:10.5281/zenodo.7426856