专利号:US-11926589-B2 优先权日:2019-07-09 标 题 :Process for the synthesis of non-racemic cyclohexenes 发明人:REISMAN SARAH; ROMBOLA MICHAEL; LADD CAROLYN L; MCLAUGHLIN MARTIN JOHN; ZUEND STEPHAN; GOETZ ROLAND 权利人:BASF CORP; CALIFORNIA INST OF TECHN 摘要:This invention relates to a process for the synthesis of a non-racemic cyclohexene compound of formula (I) by a Diels-Alder reaction of a compound of formula (II) with a compound of formula (III) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and Y have the meanings as defined in the description in the presence of a catalyst comprising at least one m-valent metal cation M m+ wherein the metal M is selected from Scandium (Sc), Yttrium (Y), Lanthanum (La), Cerium (Ce), Praseodymium (Pr), Neodymium (Nd), Promethium (Pm), Samarium (Sm), Europium (Eu), Gadolinium 15 (Gd), Terbium (Tb), Dysprosium (Dy), Holmium (Ho), Erbium (Er), Thulium (Tm), Ytterbium (Yb), Lutetium (Lu), Gallium (Ga) and Indium (In), and m is an integer of 1, 2 or 3, and a chiral ligand of the formula (IV) wherein R 10a , R 10b , R 10c , R 10d , R 10a′ , R 10b′ , R 10c′ , R 10d′ , Z and Z′ have the meanings as defined in the description.
专利号:US-11566040-B2 优先权日:2019-01-28 标题:Synthesis of O-antigen oligosaccharide compounds of Helicobacter pylori serotype O2 发明人:YIN JIAN; HU JING; LIU ZHONGHUA; QIN CHUNJUN 权利人:UNIV JIANGNAN 摘要:Disclosed is synthesis of an O-Antigen oligosaccharide compound of Helicobacter pylori serotype O2, belonging to the field of organic synthesis. The disclosure obtains O-antigen disaccharide to tetracosasaccharide of Helicobacter pylori serotype O 2 by chemical synthesis. A chemical synthesis method which is quite conducive to production of a glucose-α-lglucosidic bond is developed in the disclosure by a protectant strategy, temperature effect, solvent effect, and additive effect. The method is applied in synthesis of an O-antigen oligosaccharide compound of Helicobacter pylori serotype O2 assembled with an amino linking arm. A saccharide conjugate can be prepared from the synthesized O-antigen oligosaccharide compound of Helicobacter pylori serotype O2 assembled with an amino linking arm together with a carrier protein for immunology researches, playing an important role in preventing and treating Helicobacter pylori.
专利号:WO-2024153752-A1 优先权日:2023-01-20 标 题 :Stereoselective synthesis of intermediates and synthesis of quinagolids 发明人:RYBERG PER; PINESCHI MAURO; COMPARINI LUCREZIA 权利人:FERRING BV 摘要:Disclosed is a method for preparing compounds with improved stereoselectivities. The described compounds are useful intermediates and may find particular application in the synthesis of compounds containing an octahydrobenzoquinoline moiety (e.g. an octahydrobenzo[g]quinoline moiety), such as quinagolide and its derivatives. Also disclosed is a method for stereoselectively (e.g. enantioselectively) preparing an intermediate used in the existing manufacturing process for the synthesis of quinagolide this intermediate also finding utility in the synthesis of other compounds containing an octahydrobenzo[g]quinoline moiety, in particular those having a substituent at the 3- position on the octahydrobenzo[g]quinoline.
专利号:US-2024092821-A1 优先权日:2020-03-31 标题:Synthesis of oligonucleotides and related compounds 发明人:ZHONG MINGHONG; JIN YI; GALA DINESH; PRHAVC MARIJA 权利人:JANSSEN BIOPHARMA INC 摘要:Methods of synthesizing oligonucleotides via new intermediates on a cleavable support having an azidomethyl moiety are disclosed. The method comprises multiple reaction cycles, each of which comprises sequential coupling a nucleoside or oligonucleotide subunit on a cleavable support having an azidomethyl moiety and a nucleoside phosphoramidite or an oligonucleotide phosphoramidite, capping, oxidation/thiolation and deblocking; followed by orthogonal cleavage of the azidomethyl support while keeping all other protecting groups intact. The method can be used in combination with a support moiety for either solid phase or liquid phase oligo synthesis. The soluble support facilitates homogeneous reactions and efficient separations by simple precipitation. The methods also provide novel intermediates useful in the synthesis of oligonucleotide conjugates.
专利号:US-8680276-B2 优先权日:2009-03-06 标题 :Synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine 发明人:MOTTERLE RICCARDO; ARVOTTI GIANCARLO; BERGANTINO ELISABETTA; CASTELLIN ANDREA; FOGAL STEFANO; GALVAGNI MARCO 权利人:MOTTERLE RICCARDO; ARVOTTI GIANCARLO; BERGANTINO ELISABETTA; CASTELLIN ANDREA; FOGAL STEFANO; GALVAGNI MARCO 摘要:The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.
专利号:US-2012302756-A1 优先权日:2010-02-19 标 题 :Process for synthesis of 2-substituted pyrrolidines and piperadines 发明人:LELETI RAJENDER REDDY; LIU YUGANG; PRASHAD MAHAVIR 权利人:LELETI RAJENDER REDDY; LIU YUGANG; PRASHAD MAHAVIR 摘要:The present invention provides a highly efficient, versatile one-step process for asymmetric synthesis of either diastereomer of 2-substituted pyrrolidines from a single starting material with excellent yields and high diastereoselectivety. Also provided is a method for the asymmetric synthesis of both diastereomers of 2-substituted piperidines with good yields and excellent diastereoselectivety. Diasteroselectivity is controlled effectively by choice of reducing agent.
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