专利号:US-7576234-B2 优先权日:2002-05-15 标题 :Synthesis of 2-alkyl amino acids 发明人:CHORGHADE MUKUND S; GURJAR MUKUND K; MOHAPATRA DEBENDRA K 权利人:GENZYME CORP 摘要:Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.
专利号:US-9493409-B2 优先权日:2013-04-04 标题 :Process for the synthesis of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine 发明人:ZUPANCIC BORUT 权利人:LEK PHARMACEUTICALS 摘要:The present invention provides new intermediate compounds or formulae (III) and (IVa), and salts thereof, and their use in a new synthetic process for the production of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine (vortioxetine) an experimental drug under development for the treatment of depression and anxiety.
专利号:US-2005095280-A1 优先权日:2003-10-15 标 题:Single-component pH-sensitive liposomes of reduced solid-to-liquid phase transition temperatures 发明人:SAVVA MICHALAKIS 权利人:MICHALAKIS SAVVA 摘要:The current invention relates to the synthesis of novel cationic lipids and their use as delivery vectors for nucleic acids, peptides and other synthetic drugs, in vitro and in vivo. The cationic lipids described herein form stable lamellar structures (liposomes) at physiological pH but destabilize to micelles at acidic and alkaline pH. These structures are characterized of high elasticity, increased fluidity and high transfection activity relative to the corresponding 1,2-dialkyl cationic derivatives and other phospholipids analogues.
专利号:US-9944579-B2 优先权日:2015-01-15 标题 :Catalytic hydrogenation process for the synthesis of terminal diols from terminal dialkyl aliphatic esters 发明人:BALARAMAN EKAMBARAM; SAHOO MANOJ KUMAR 权利人:COUNCIL SCIENT IND RES 摘要:A phosphorus ligand-free, mild, efficient and complete catalytic hydrogenation process is for the sustainable production of terminal diols from renewable terminal dialkyl esters with improved yield. Soluble, phosphorus ligand free Ru (II)-pincer type complexes can be used as catalysts in the hydrogenation process.
专利号:US-2021402380-A1 优先权日:2020-06-23 标 题 :Perovskites for photocatalytic organic synthesis 发明人:YAN YONG 权利人:SAN DIEGO STATE UNIV FOUNDATION 摘要:Nature is capable of storing solar energy in chemical bonds via photosynthesis through a series of C—C, C—O and C—N bond-forming reactions starting from CO 2 and light. Direct capture of solar energy for organic synthesis is a promising approach. Lead (Pb)-halide perovskite solar cells reach 24.2% power conversion efficiency, rendering perovskite a unique type material for solar energy capture. We show that photophysical properties of perovskites is useful in photoredox organic synthesis. Because the key aspects of these two applications are both relying on charge separation and transfer. Here we demonstrated that perovskites nanocrystals are exceptional candidates as photocatalysts for fundamental organic reactions, i.e. C—C, C—N and C—O bond-formations. Stability of CsPbBr 3 in organic solvents and ease-of-tuning their bandedges garner perovskite a wider scope of organic substrate activations.
专利号:US-2003236435-A1 优先权日:2002-05-15 标题 :Synthesis of 2-alkylcysteine via substituted thiazoline ester
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合成参考文献
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