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.
专利号:US-8383810-B2 优先权日:2004-12-20 标题:Process for the synthesis of azetidinones 发明人:THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L 权利人:MERCK SHARP & DOHME; THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L 摘要:A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.
专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
专利号:US-7129357-B2 优先权日:2003-09-15 标题:Synthesis of quinoline 5-carboxamides useful for the preparation of PDE IV inhibitors 发明人:ANDREWS DAVID R; TANG SUHAN; WU WENXUE; KALLINEY SAMI Y; SUDHAKAR ANANTHA; NIELSEN CHRISTOPHER 权利人:SCHERING CORP 摘要:In one embodiment, the present application discloses a process for making the compound of the formula:
专利号:US-2011152313-A1 优先权日:2008-06-20 标题 :Synthesis of ageladine a and analogs thereof 发明人:KARUSO PETER HELMUTH; SHENGULE SUDHIR RAMNATHRAO 权利人:UNIV MACQUARIE 摘要:The invention describes a one pot process for synthesizing a compound of structure (I), or a tautomer thereof. A compound of structure (II), or a tautomer thereof, and an aldehyde of structure R d CHO are condensed to form a condensation product. The resulting condensation product is then oxidized in the same reaction mixture to produce the compound of structure (I) or a tautomer thereof.
专利号:WO-2024134682-A1 优先权日:2022-12-21 标题:(n-alkyldihydrol-2h-oxazinyl)-cannabidiol as anti-proliferative agent and process for preparation thereof 发明人:CHAM PANKAJ SINGH; SINGH AJEET; JAMWAL ASHIYA; SINGH RATTANDEEP; - SHABU; THAPA SONIA; WAZIR PRIYA; NANDI UTPAL; SINGH SHASHANK KUMAR; SINGH PARVINDER PAL 权利人:COUNCIL OF SCIENT AND INDUSTRIAL RESEARCH AN INDIAN REGISTERED BODY INCORPORATED UNDER THE REGN OF S 摘要:The present invention relates to ring annulated analogues of cannabidiol where either one or both sides of the aromatic ring are attached to the oxazinyl ring, their method of preparation and use as anti-proliferative agents. The present invention provides a ring annulated cannabidiol analogue compound of Formula I. The present invention further provides a process for the synthesis of ring annulated cannabidiol analogue compound of Formula I.
[参考文献]: Byeong Kwon Park, Et Al. Tetra-μ-Benzoato-Bis-[参考文献]: S Schach, Et Al. Microbial Metabolism Of Quinoline And Related Compounds. Xvii. Degradation Of 3-Methylquinoline By Comamonas Testosteroni 63. Biol Chem Hoppe Seyler. 1993 Mar;374(3):175-81. [参考文献]: Tamara Rodríguez-Cabo, Et Al. Time-Of-Flight Accurate Mass Spectrometry Identification Of Quinoline Alkaloids In Honey. Anal Bioanal Chem. 2015 Aug;407(20):6159-70.
合成参考文献
参考文献:10.1107/s1600536811007021 摘要:Hyun MY, Kim P, Kim C, Kim Y. catena-Poly[[tetraaqua[trans-1,2-bis(4-pyridyl)ethene-κ2N:N′]nickel(II)] dinitrate]. Acta Crystallogr E Struct Rep Online. 2011 Mar 02;67(4):m390. doi: 10.1107/s1600536811007021.