专利号:US-2025171493-A1 优先权日:2022-03-05 标题 :Processes for synthesis of withanolides and withaferins and analogs thereof 发明人:LOPCHUK JUSTIN MATTHEW 权利人:H LEE MOFFITT CANCER CT & RES 摘要:The present disclosure provides processes for the synthesis of withanolides such as Withanolide A and Withanolide D.
专利号:US-2024199680-A1 优先权日:2021-04-02 标 题:Synthesis of fluorinated cyclic dinucleotides 发明人:AN CHIHUI; FIER PATRICK S; HIRAGA KAORI; LIU ZHIJIAN; MARSHALL NICHOLAS M; MCINTOSH JOHN; MILLER STEVEN P; MOORE JEFFREY C; MURPHY GRANT S; OBLIGACION JENNIFER V; PAN WEILAN; PENG FENG; SALEHI MARZIJARANI NASTARAN; WINSTON MATTHEW S 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated cyclic dinucleosides, such as [P(R)]-2′-deoxy-2′-fluoro-5′-O—[(R)-hydroxymercaptophosphinyl]-P-thio-β-D-arabino-adenylyl-(3′→5′)-3′-deoxy-3′-fluoroguanosine cyclic nucleotide, which is also known as (2R,5R,7R,8S,10R,12aR,14R,15S,15aR,16R)-7-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-14-(6-amino-9H-purin-9-yl)-15,16-difluoro-2, 10-bis(sulfanyl)octahydro-2H,10H, 12H-2λ 5 ,10λ 5 -5,8-methanofuro[3,2-1][1, 3,6,9,11,2,10]pentaoxadiphosphacyclotetradecine-2,10-dione. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
专利号:US-4355184-A 优先权日:1980-05-02 标题:Synthesis of α, β-unsaturated-ketones 发明人:KAKU TSUTOMU; KATSUURA KIYOSHI; SAWAKI MIKIO 权利人:NIPPON SODA CO 摘要:alpha , beta -unsaturated-ketones are synthesized by reacting with an aldehyde and an alkali metal salt of acetoacetic acid in the presence of an aliphatic secondary amine in the mixture of heterogeneous solvents producing an oil layer and a water layer.
专利号:US-5565517-A 优先权日:1994-11-16 标题:Synthesis of organic polysulfide polymers 发明人:EFNER HOWARD F; SHAW JAMES E 权利人:PHILLIPS PETROLEUM CO 摘要:A process for preparing an organic polysulfide polymer, such as polyethylene trisulfide, is provided which comprises contacting a dimercaptan such as 1,2-ethanedithiol with elemental sulfur using a basic catalyst wherein the dimercaptan, elemental sulfur, and basic catalyst are each present in an effective amount to effect the preparation of the organic polysulfide polymer. A process for controlling the molecular weight of an organic polysulfide polymer is also provided which comprises contacting a mercaptan with a dimercaptan and sulfur, in the presence of a basic catalyst, under conditions sufficient to prepare an organic polysulfide polymer.
专利号:US-7718598-B1 优先权日:1998-09-25 标 题:Auxiliary for amide bond formation 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programmes. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganizing peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-8227622-B2 优先权日:2009-07-06 标题:Pharmaceutical process and intermediates 714 发明人:AINGE DEBRA; MERIFIELD ERIC; THOMSON COLIN; BUTTERS MICHAEL; RAMAKRISHNAN RAVI; RAYAPATI RAVI NAIDU; SHARMA PARHALAD RAY 权利人:AINGE DEBRA; MERIFIELD ERIC; THOMSON COLIN; BUTTERS MICHAEL; RAMAKRISHNAN RAVI; RAYAPATI RAVI NAIDU; SHARMA PARHALAD RAY; ASTRAZENECA AB 摘要:The invention relates to compounds of formula (X), and salts thereof, and their use as intermediates in improved manufacturing processes for the synthesis of pharmaceutical compound (I): n n n n n n n n n n X is â•?O, â•?N—OH or â•?N—OC(O)Me; Y is hydrogen, PhS- or p-chlorophenylsulfanyl; Z is hydrogen or —CH 2 COOR 1 wherein R 1 is selected from hydrogen, optionally substituted hydrocarbyl and optionally substituted heterocyclyl.
[参考文献]: D I Draganov, Et Al. Rabbit Serum Paraoxonase 3 (Pon3) Is A High Density Lipoprotein-Associated Lactonase And Protects Low Density Lipoprotein Against Oxidation. J Biol Chem. 2000 Oct 27;275(43):33435-42. [参考文献]: Yu Yuan, Et Al. Toward Homogeneous Erythropoietin: Fine Tuning Of The C-Terminal Acyl Donor In The Chemical Synthesis Of The Cys29-Gly77 Glycopeptide Domain. J Am Chem Soc. 2009 Apr 22;131(15):5432-7.
合成参考文献
摘要:Petasis, N. A., Science of Synthesis, (2010) 47, 225. 摘要:Shimizu, M., Science of Synthesis Knowledge Updates, (2010) 3, 25. 摘要:Cellnik, T.; Jo, W.; Healy, A., Science of Synthesis: Knowledge Updates, (2024) 2, 371. 摘要:Cellnik, T.; Jo, W.; Healy, A., Science of Synthesis: Knowledge Updates, (2024) 2, 345. 摘要:Cellnik, T.; Jo, W.; Healy, A., Science of Synthesis: Knowledge Updates, (2024) 2, 366.