专利号:US-2019292219-A1 优先权日:2018-03-26 标 题:Method of solid-state peptide synthesis using a novel polymeric support 发明人:JERABEK KAREL; HANKOVA LIBUSE; HOLUB LADISLAV; ZECCA MARCO; CENTOMO PAOLO; TROVO DANIELE; LEDER RICCARDO; BIONDI BARBARA 权利人:INST OF CHEMICAL PROCESS FUNDAMENTALS OF THE CAS V V I; UNIV DEGLI STUDI PADOVA 摘要:A method of solid-state synthesis of peptides that provides a polymeric solid-state synthesis support, attaches a first amino acid to said support to form the first amino acid molecule of the desired peptide chain, attaches additional amino acids to form the desired peptide chain, characterized in that the polymeric solid-state synthesis support is a styrenic polymer containing at least 50 mol % divinylbenzene monomer units, the styrenic polymer being functionalized with chloromethyl and/or benzyloxybenzyl alcohol and/or amino moieties, and having porosity 60-90% and medium pore diameter ranging from 10 to 80 nm. A functionalized styrenic polymer is claimed.
专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:WO-2009018504-A1 优先权日:2007-08-01 标题 :Process for the synthesis of diaminopyridine and related compounds 发明人:RITTER JOACHIM C 权利人:DU PONT; RITTER JOACHIM C 摘要:A process is provided for the synthesis of a diaminopyridine, such as 2,6-diaminopyridine and related compounds, which are used industrially as compounds and as components in the synthesis of a variety of useful materials. The synthesis proceeds by means of a chlorine-ammonia displacement in the presence of a copper source.
专利号:US-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:US-7479569-B2 优先权日:2004-02-13 标题:Process for the synthesis of (7-methoxy-3,4-dihydro-1-naphthalenyl) acetonitrile and its application in the synthesis of agomelatine 发明人:SOUVIE JEAN-CLAUDE; GONZALEZ BLANCO ISAAC 权利人:SERVIER LAB 摘要:A process for the industrial synthesis of the compound of formula (I) n nApplication in the synthesis of agomelatine.
专利号:US-7999129-B2 优先权日:2004-02-13 标 题:Process for the synthesis of (7-methoxy-1-naphthyl) acetonitrile and its application in the synthesis of agomelatine 发明人:SOUVIE JEAN-CLAUDE; BLANCO ISAAC GONZALEZ 权利人:SERVIER LAB 摘要:A process for the industrial synthesis of the compound of formula (I) n nApplication in the synthesis of agomelatine.
参考文献:10.1155/2011/238513 摘要:Franko J, Jackson LG, Meade BJ, Anderson SE. Allergic Potential and Immunotoxicity Induced by Topical Application of 1-Chloro-4-(Trifluoromethyl)Benzene (PCBTF) in a Murine Model. J Allergy (Cairo). 2011;2011():238513. 参考文献:10.1007/s00248-011-9906-8 摘要:Graças DA, Miranda PR, Baraúna RA, McCulloch JA, Ghilardi R, Schneider MP, Silva A. Microbial diversity of an anoxic zone of a hydroelectric power station reservoir in Brazilian Amazonia. Microb Ecol. 2011 Nov;62(4):853–61. doi: 10.1007/s00248-011-9906-8.