专利号:US-8710268-B2 优先权日:2007-07-31 标题:Method for the hydrolysis of substituted formylamines into substituted amines 发明人:BOBYLEV MIKHAIL 权利人:BOBYLEV MIKHAIL 摘要:An improved method for the synthesis of substituted formylamines and substituted amines via an accelerated Leuckart reaction. The Leuckart reaction is accelerated by reacting formamide or N-alkylformamide and formic acid with an aldehyde or a ketone at a preferred molar ratio that accelerates the reaction. The improved method is applicable to various substituted aldehydes and ketones, including substituted benzaldehydes. An accelerated method for the hydrolysis of substituted formylamines into substituted amines using acid or base and a solvent at an elevated temperature. The improved method is useful for the accelerated synthesis of agrochemicals and pharmaceuticals such as vanillylamine, amphetamine and its analogs, and formamide fungicides.
专利号:US-7785564-B2 优先权日:2002-07-27 标 题 :Design and synthesis of renal dipeptidase inhibitors 发明人:KHAN SAEED R; VOGELSTEIN BERT; KINZLER KENNETH W; GURULINGAPPA HALLUR; BUCKHAULTS PHILLIP 权利人:UNIV JOHNS HOPKINS 摘要:Aminophosphinic acid derivatives were synthesized as potential inhibitors of renal dipeptidase, an enzyme overexpressed in benign and malignant colon tumors. Several compounds showed potent enzyme-inhibitory activity. These compounds can be used therapeutically and diagnostically for treatment and detection of tumors.
专利号:US-6180767-B1 优先权日:1996-01-11 标 题 :Peptide nucleic acid conjugates 发明人:WICKSTROM ERIC; BASU SOUMITRA 权利人:UNIV JEFFERSON 摘要:Peptide nucleic acid (PNA) oligomers are conjugated to a ligand which is capable of binding to a cell surface receptor. The ligand facilitates cellular uptake of the PNA oligomer. Where the ligand is a peptide, the conjugate may be produced as a unitary molecule by first synthesizing the peptide ligand by solid phase or solution peptide synthesis, followed by synthesis of the PNA oligomer as an extension of the peptide ligand. The PNA oligomer base sequence is selected to hybridize to a target polynucleotide sequence by either triplex (dsDNA) or duplex (ssDNA; RNA) formation.
专利号:US-10669306-B2 优先权日:2016-02-04 标题:Solid supports for use in solid-phase peptide synthesis, kits, and related methods 发明人:CHATTERJEE CHAMPAK; SHELTON PATRICK M; WELLER CAROLINE E 权利人:UNIV WASHINGTON 摘要:Solid supports for use in solid-phase peptide synthesis (SPPS) are provided. The solid supports may include a resin and a protected linker coupled to the resin. The linker may be an N-mercaptoethoxyglycine, an N-mercaptopropoxyglycine, an N-mercaptobutoxyglycine, and/or another suitable linker. Kits for use in SPPS are also provided. The kits may include a solid support, a solution including a thiol or a selenol, one or more pluralities of protected amino acids, and/or a wash buffer. Methods of SPPS are also provided. The methods may include providing a solid support including a resin coupled to a protected linker.
专利号:US-8703747-B2 优先权日:2008-07-23 标题 :Aminophosphinic derivatives that can be used in the treatment of pain 发明人:ROQUES BERNARD; PORAS HERVÉ; FOURNIE-ZALUSKI MARIE-CLAUDE 权利人:ROQUES BERNARD; PORAS HERVÉ; FOURNIE-ZALUSKI MARIE-CLAUDE; PHARMALEADS 摘要:The present invention relates to a compound of the following general formula (I): R 1 —NH—CH(R 2 )—P(â•?O)(OR 3 )—CH 2 —C(R 4 )(R 5 )—CONH—CH(R 6 )—COOR 7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R 1 represents a —C(â•?O)—O—C(R 8 )(R 9 )—OC(â•?O)—R 10 group; R 2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R 3 represents a hydrogen atom or a —C(R 12 )(R 13 )—OC(â•?O)—R 14 group; R 4 and R 5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R 4 represents a hydrogen atom and R 5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R 6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substituted; and R 7 represents a hydrogen atom or a benzyl, alkyl, heteroaryl, alkylheteroaryl, —CHMe—COOR 18 , —CHR 19 —OC(â•?O)OR 20 and —CHR 19 —OC(â•?O)OR 20 group. The present invention also relates to the use of these compounds as a medicinal product, and in particular for the treatment of pain, more avantageously neuropathic and neuroinflammatory pain, to their method of synthesis and also to the compositions containing them.
专利号:US-12391710-B2 优先权日:2019-12-11 标 题 :Method for the industrial preparation of the disodium salt of ((2S)-3-([1,1′-biphenyl]-4-yl-2-((hydroxy((1R)-1-(((1-(isobutyryloxy)ethoxy)carbonyl)amino)ethyl)phosphoryl) methyl)propanoyl)-l-alanine 发明人:PORAS HERVÉ; PRIOUR ALAIN; GRACH GUILLAUME; FANELLI ROBERTO; ZHAO XINJUN 权利人:PHARMALEADS; KOS THERAPEUTICS INC 摘要:The present invention relates to a method for the industrial preparation of ((2S)-3-([1,1′-biphenyl]-4-yl)-2-((((R)-1-aminoethyl)(hydroxy)phosphoryl)methyl)propanoyl)-L-alanine acid of following formula (E):from (S)-1-phenylethylamine via a multi-step synthesis.The present invention pertains to a method for the industrial preparation of the disodium salt of ((2S)-3-([1,1′-biphenyl]-4-yl)-2-((hydroxy((1R)-1-(((1-(isobutyryloxy)ethoxy)carbonyl)amino)ethyl)phosphoryl)methyl)propanoyl)-L-alanine of following formula (1):in two additional steps from the compound (E) such as defined above.The present invention also pertains to a method for diastereoisomeric enrichment of the intermediates of the method for the industrial preparation of the compound of formula (E) of the present invention.
摘要:Wang, S.-H.; Tu, Y.-Q.; Tang, M., Science of Synthesis: Applications of Domino Transformations in Organic Synthesis, (2015) 1, 277. 摘要:Kiyokawa, K., Science of Synthesis: Hypervalent Halogens in Organic Synthesis, (2025) .