专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
专利号:US-9126995-B2 优先权日:2011-11-08 标题:Method for catalytic asymmetric synthesis of optically active isoxazoline compound and optically active isoxazoline compound 发明人:TOYAMA KEN-ICHI; MORIYAMA YUJI; MATOBA KAZUTAKA; YAOSAKA MANABU; IKEDA EITATSU 权利人:NISSAN CHEMICAL IND LTD 摘要:There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an α,β-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method.
专利号:US-2024024489-A1 优先权日:2020-11-20 标 题:Protected disaccharides, their process of preparation and their use in the synthesis of zwitterionic oligosaccharides, and conjugates thereof 发明人:MULARD LAURENCE; DHARA DEBASHIS; PFISTER HELENE; PAOLETTI JULIE; PHALIPON ARMELLE; GUERREIRO-INVERNO CATHERINE 权利人:PASTEUR INSTITUT 摘要:The present invention provides zwitterionic oligosaccharides, in particular fragments of the surface polysaccharides from Shigella sonnei and Shigella sonnei conjugates comprising them. The present invention also provides protected disaccharides, their process of preparation and their use in the synthesis of zwitterionic oligosaccharides, and conjugates thereof, the disaccharide repeating unit of Shigella sonnei being: (I)
专利号:US-10793495-B2 优先权日:2015-08-14 标 题:Synthesis of polyaryl substituted aryl compounds 发明人:BOULOS RAMIZ; FEUTRILL JOHN 权利人:BOULOS & COOPER PHARMACEUTICALS PTY LTD 摘要:A method for the synthesis of a aryl compound of Formula (1).n nU T-W—R 1 ) n    (1)
专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:US-9676814-B2 优先权日:2013-10-01 标题:Industrial process for the synthesis of ulipristal acetate and its 4′-acetyl analogue 发明人:Mahó Sándor; SÃ?NTA CSABA; Csörgei János; Horváth János; ARANYI ANTAL; BÉNI ZOLTÃ?N 权利人:RICHTER GEDEON NYRT 摘要:The present invention relates to a new process for the synthesis of compounds of formula (I) (wherein the meaning of R is dimethylamino or acetyl group) using the compound of formula (II) (wherein the meaning of R is dimethylamino or 2-methyl-1,3-dioxolan-2-yl group) as starting material, as well as to the intermediate of the process.
[参考文献]: A Closse, Et Al. Binding Studies With [参考文献]: C Moret, Et Al. Potency Ratio For The Inhibition Of 3H-Qnb And 3H-Cis-Methyldioxolane Binding Predicts Agonist Or Antagonist Activity On Muscarinic Receptors. Methods Find Exp Clin Pharmacol. 1988 Oct;10(10):619-21. [参考文献]: H Tecle, Et Al. Synthesis And Sar Of Bulky 1-Azabicyclo[参考文献]: J B Galper, Et Al. Muscarinic Cholinergic Receptors In The Embryonic Chick Heart: Interaction Of Agonist, Receptor, And Guanine Nucleotides Studied By An Improved Assay For Direct Binding Of The Muscarinic Agonist [参考文献]: J Velazquez-Moctezuma, Et Al. Cholinergic Antagonists And Rem Sleep Generation. Brain Res. 1991 Mar 8;543(1):175-9.
合成参考文献
摘要:Bietti, M.; Dénès, F., Science of Synthesis, (2021) , 504. 摘要:Gigiena i Sanitariya. For English translation, see HYSAAV., 39(11)(94), 1974 摘要:Gigiena i Sanitariya. For English translation, see HYSAAV., 47(8)(89), 1982