专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-7714063-B2 优先权日:2007-11-15 标 题 :Solid support for Fmoc-solid phase synthesis of peptides 发明人:SRIVASTAVA KRIPA SHANKER; DAVIS MATTHEW RYAN 权利人:MALLINCKRODT INC 摘要:The present invention provides compositions and processes for the solid phase synthesis of polypeptides. In particular, the present invention provides solid supports and processes for preparing solid supports for the synthesis of polypeptides.
专利号:WO-2004037772-A1 优先权日:2002-10-22 标 题 :Convenient and scalable synthesis of ethyl n-[(2-boc-amino) ethyl] glycinate and its hydrochloride salt 发明人:HUDSON ROBERT H E; VIIRRE RUSSELL D 权利人:UNIV WESTERN ONTARIO; HUDSON ROBERT H E; VIIRRE RUSSELL D 摘要:The present invention discloses an improved synthesis of ethyl N-[(2-Boc-amino)ethyl]glycinate and its hydrochloride salt. The synthesis is based on the reductive alkylation of Boc-ethylenediamine with ethyl glyoxylate hydrate and furnishes the title compound in near quantitative yield and high purity without chromatography. This compound is suitable, as is, for the synthesis peptide nucleic acid monomers. Further, conversion to the hydrochloride salt provides a stable, non-hygroscopic solid that is a convenient form for handling and storage.
专利号:WO-2023019298-A1 优先权日:2021-08-20 标 题:Improved method of synthesis of 1-(3',4'-methylene dioxyphenyl)-2-(methylamino) propane (mdma) 发明人:O'MALLEY WILLIAM IAN; WYNNE PAUL MICHAEL 权利人:MIND MEDICINE AUSTRALIA LTD 摘要:The present invention relates to an improved method of synthesis of 1-(3',4'-methylenedioxyphenyl)-2-(methylamino)propane (MDMA) that is of sufficient purity that it can be used for pharmaceutical applications. In particular the present invention provides a method of synthesising MDMA comprising the steps of (a) condensation of piperonal and nitroethane in the presence of a catalysing base to form 1-(3',4'-methylenedioxyphenyl)-2-nitroprop-1-ene (MDP-2-nitropropene), (b) oxidative hydrolysis of MDP-2-nitropropene to form 1-(3',4'methylenedioxyphenyl)-propan-2-one (MDP2P), and (c) reductive amination of MDP2P to 1-(3',4'-methylenedioxyphenyl)-2-(methylamino)propane (MDMA).
专利号:US-5723619-A 优先权日:1997-01-13 标 题 :Method for the synthesis of deoxypyridinoline 发明人:HATCH ROBERT P 权利人:BAYER AG 摘要:Disclosed is a method for the chemical synthesis of deoxypyridinoline (DPD). The synthesis involves the preparation of a protected 3-hydroxypyridinium starting with a Nα-protected lysine and a 5,6-epoxy-2-N-protected-O-protected-(2S)-2-aminohexanoate with subsequent deprotection to provide the desired DPD.
专利号:US-9630923-B2 优先权日:2013-07-09 标题:Biocatalyzed synthesis of the optically pure (R) and (S) 3-methyl-1,2,3,4-tetrahydroquinoline and their use as chiral synthons for the preparation of the antithrombic (21R)- and (21S)-argatroban 发明人:GRISENTI PARIDE 权利人:EUTICALS SPA; EUTICALS SPA 摘要:The present invention relates to the biocatalyzed synthesis of enantiomerically pure (3R) and (3S)-methyl-1,2,3,4-tetrahydroquinoline. Said enantiomerically pure compounds are useful as chiral synthons in organic synthesis and, in particular, for the preparation of diastereomerically pure (21R) and (21S)-agratroban and its analogs. New compounds used as intermediates in the process of the invention are also disclosed.
参考标题:A Convenient Route To Azetidine-2,3-Diones And Cis-3β-Amido Azetidinones 作者:Joseph J. Tufariello,Donald J.P. Pinto,Arnold S. Milowsky,Daniel V. Reinhardt |发布日期:1987.1 摘要:The Synthesis Of 3β-Amido Azetidinones, 8A And 8B, Via Azetidine-2,3-Diones Is Described.
合成参考文献
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