专利号:US-5877278-A 优先权日:1992-09-24 标题:Synthesis of N-substituted oligomers 发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
专利号:US-9242925-B2 优先权日:2011-08-29 标题:Versatile and stereospecific synthesis of γ,δ-unsaturated amino acids by Wittig reaction 发明人:JUGE SYLVAIN; BAYARDON JEROME; REMOND EMMANUELLE; ONDEL-EYMIN MARIE-JOELLE 权利人:JUGE SYLVAIN; BAYARDON JEROME; REMOND EMMANUELLE; ONDEL-EYMIN MARIE-JOELLE; CENTRE NAT RECH SCIENT; UNIV BOURGOGNE 摘要:The γ,δ-unsaturated α-amino acids of general formula (I). Also, a versatile process for the stereospecific synthesis of said compounds of formula (I), involving a Wittig reaction. Further, intermediate products of general formulae (II) and (III), as shown below, which are involved in the synthesis of compounds (I). n n n n n n n n n n n n Compounds of general formula (I) may be useful as therapeutic substances, or as reagents or intermediates for fine chemistry.
专利号:US-11168050-B2 优先权日:2014-03-27 标 题 :Efficient synthesis of amines and amides from alcohols and aldehydes by using cascade catalysis 发明人:CÓRDOVA ARMANDO; BERGLUND PER; ANDERSON MATTIAS; AFEWERKI SAMSON 权利人:XP CHEMISTRIES AB 摘要:The present invention relates generally to an eco-friendly methodology for the conversion of alcohols and aldehydes to amines and amides using an integrated enzyme cascade system with metal- and organocatalysis. More specifically, the present invention relates to synthesis of capsaicinoids starting from vanillin alcohol and using a combination of an enzyme cascade system and catalysts. Furthermore, the method also relates to synthesis of capsaicinoids derivatives starting from vanillin alcohol derivatives and using a combination of an enzyme cascade system and catalysts.
专利号:US-9724673-B2 优先权日:2011-06-30 标 题:Supported alkoxylated organotin reactant, preparation and use for heterogeneous-phase synthesis of tetrazoles 发明人:LE GROGNEC ERWAN; QUINTARD JEAN-PAUL; KERRIC GAELLE; CHRETIEN JEAN-MATHIEU; ZAMMATTIO FRANCOISE 权利人:LE GROGNEC ERWAN; QUINTARD JEAN-PAUL; KERRIC GAELLE; CHRETIEN JEAN-MATHIEU; ZAMMATTIO FRANCOISE; UNIV NANTES; CENTRE NAT RECH SCIENT 摘要:A supported alkoxylated organotin reactant, to the process for preparing same, to the use of such a reactant as a catalyst for heterogeneous-phase organic synthesis, and also to a process for heterogeneous-phase synthesis of 5-substituted or 1,5-disubstituted tetrazoles using such a reactant.
专利号:WO-2015193910-A1 优先权日:2014-06-20 标题:Asymmetric synthesis of 2-substituted indolines and 3-substituted cinnolines 发明人:KUMAR BOOPATHY SENTHIL; SUDALAI ARUMUGAM 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to a novel one step proline catalyzed process for synthesis of chiral hydrazine and its derivatives from o-bromo hydro cinamaldehyde. Further, it relates to a novel one step process for the synthesis of substitued indolines and cinnolines from chiral hydrazines and its derivatives.
专利号:US-10040752-B2 优先权日:2015-08-24 标 题 :Synthesis of levomethadone hydrochloride or dextromethadone hydrochloride and methods for use thereof 发明人:MKRTCHYAN GNEL; YAO QINGWEI 权利人:CODY LABORATORIES INC 摘要:Highly efficient methods for synthesis of levomethadone hydrochloride or dextromethadone hydrochloride are provided starting from D-alanine, or L-alanine, respectively, with retention of configuration. Methods for treating a subject are provided comprising administering a composition comprising an effective amount of levomethadone hydrochloride having not more than 10 ppm dextromethadone.
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合成参考文献
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