专利号:US-2007015260-A1 优先权日:2002-03-14 标 题:Synthesis of synthons for the manufacture of bioactive compounds 发明人:WONG CHI-HUEY; LIU JUNJIE; DESANTIS GRACE; BURK MARK 权利人:SCRIPPS RESEARCH INST 摘要:The present invention is based on the discovery that 2-deoxyribose-5-phosphate aldolase (DERA, EC 4.1.2.4) and variants thereof can be used to catalyze sequential asymmetric aldol reactions between a wide variety of donor and acceptor aldehydes. The reaction products typically contain at least two new stereogenic centers and can be produced in enantiomerically pure form. As such, DERA catalyzed asymmetric aldol chemistry can be exploited to produce synthons for the synthesis of a variety of bioactive molecules.
专利号:US-9422216-B2 优先权日:2012-08-27 标 题:Method for synthesis of lactic acid and its derivatives and catalyst for preparing same 发明人:ZHOU XIAOPING 权利人:MICROVAST POWER SYSTEMS CO LTD; MICROVAST POWER SYSTEMS CO LTD 摘要:The present disclosure provides a catalyst for preparing lactic acid and derivatives thereof, comprising at least one of metallic compounds MX n , wherein M is selected from Na, K, Mg, Ca, Sr, Ba, Al, Ga, In, Sn, Sb, Bi, Cr, Mn, Fe, Co, Ni and Zn, and n is an integer of 1 to 6. The present disclosure further provides a method for synthesis of lactic acid and derivatives thereof, wherein at least one raw material including carbohydrates, at least one alcohol, at least one of the aforesaid catalysts and at least one solvent are heated to react to prepare lactic acid and derivatives thereof.
专利号:US-9096519-B2 优先权日:2013-01-10 标 题 :Process for the synthesis of ketones from internal alkenes 发明人:MORANDI BILL; GRUBBS ROBERT H; WICKENS ZACHARY K; LERCH MICHAEL M 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention is directed to methods for oxidizing internal olefins to ketones. In various embodiments, each method comprising contacting an organic substrate, having an initial internal olefin, with a mixture of (a) a biscationic palladium salt; and (b) an oxidizing agent; dissolved or dispersed in a solvent system to form a reaction mixture, said solvent system comprising at least one C 2-6 carbon nitrile and optionally at least one secondary alkyl amide, said method conducted under conditions sufficient to convert at least 50 mol % of the initial internal olefin to a ketone, said ketone positioned on a carbon of the initial internal olefin. The transformation occurs at room temperature and shows wide substrate scope. Applications to the oxidation of seed oil derivatives and a bioactive natural product are described.
专利号:US-2003180804-A1 优先权日:2001-10-29 标题:Solid phase synthesis of chemical libraries 发明人:PRYOR KENT E; LEWIS RONALD D; BROWN JASON W 权利人:CORVAS INT INC 摘要:The present invention provides compounds and compound libraries that are useful as protease modulators. The compounds and compound libraries are preferably made using the methods of the present invention which utilize peptide synthesis and combinatorial chemistry methods on a solid phase.
专利号:WO-2014148928-A1 优先权日:2013-03-21 标 题:Method for incorporating protecting acetal and acetal ester groups, and its application for the protection of hydroxyl function 发明人:MARKIEWICZ WOJCIECH; TOÅš-MARCINIAK AGNIESZKA; CHMIELEWSKI MARCIN 权利人:INST CHEMII BIOORG POLSKIEJ AKADEMII NAUK 摘要:The present invention is the method for incorporation of acetal and acetal ester groups for protection of hydroxyl function. The method is applied in particular in the processes of RNA synthesis. The method can be employed in the synthesis of nucleosides with acetal and acetal ester groups for the protection of hydroxyl functions. The method according to the invention consists of the reaction of an organic compound containing at least one hydroxyl group, soluble in an aprotic solvent, with a compound of the general formula 1, R 1 -S-CH 2 -O-R 2 (1) in the presence of SnCl 4 , in an aprotic solvent. In the second aspect, the present invention is the method of protecting the hydroxyl function, particularly in position 2', in nucleoside derivatives, based on the incorporation of an acetal or acetal ester group.
专利号:US-2024308991-A1 优先权日:2021-01-15 标 题:Process for the synthesis of reactive carbohydrates including antigen precursors for conjugation with a carrier material 发明人:SHIAO TZE CHIEH; MIGNANI SERGE; MOFFETT SERGE; VISHWAKARMA RAM 权利人:KORANEX CAPITAL 摘要:Carbohydrate of Formula (A)where R1 is H and n an integer from 1 to 5, is synthesized by reacting, under heating, compound (A0)with HO—(CH2)n—CHâ•?CH2 in the presence of an acid capable of liberating a proton, and cooling the reaction mixture to obtain a cooled mixture comprising compound (A).Carbohydrate of Formula (AAPG)where R2 is a monovalent protecting group, PG is a divalent protecting group and n an integer from 1 to 5, is synthesized by reacting, in the presence of a metal-containing zeolite, compound of Formula (APG)with compound of Formula (A1)where X is —I, —Br, —Cl, —CN, —OTf (Triflate), —OMs (Mesylate), —OTs (Tosylate), methylsulfate, or trichloroacetimidate. Deprotection of compound (AAPG) forms compound (AA)Carbohydrates (A) and (AA) can be coupled with a thiolated linker to form glycoconjugate precursors, which in turn are conjugatable with a carrier material such as a protein, peptide or polypeptide.
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合成参考文献
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