专利号:WO-2011106929-A1 优先权日:2010-03-02 标题:Inhibitors of hepatitis c virus ns5b polymerase 发明人:MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO 权利人:MERCK SHARP & DOHME; ANGELETTI P IST RICHERCHE BIO; MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO 摘要:Compounds of formula I that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infection and for inhibiting HCV viral replication and /or viral production in a cell-based system.
专利号:US-10865163-B2 优先权日:2017-12-20 标题:Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds 发明人:YOUNG MICHAEL C; KAPOOR MOHIT 权利人:UNIV TOLEDO 摘要:Methods of synthesizing compounds using CO 2 as a directing group for C—H functionalization, and compounds made thereby, are described.
专利号:US-2012328569-A1 优先权日:2010-03-02 标题:Inhibitors of hepatitis c virus ns5b polymerase 发明人:MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO; NARJES FRANK; HABERMANN JOERG; KOCH UWE; LIU SHILAN 权利人:MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO; NARJES FRANK; HABERMANN JOERG; KOCH UWE; LIU SHILAN 摘要:Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-2019185392-A1 优先权日:2017-12-20 标 题 :Carbon Dioxide as a Directing Group for C-H Functionalization Reactions Involving Lewis Basic Amines, Alcohols, Thiols, and Phosphines for the Synthesis of Compounds
专利号:US-6759551-B1 优先权日:2000-11-03 标题:Chiral (s- or r-methylphenylglycine) amino acid crystal and method for preparing same 发明人:PELTA ISABELLE; MARET JEAN-CLAUDE 权利人:BAYER CROPSCIENCE SA 摘要:The invention concerns chiral amino acid, is preparation method, and the use of said chiral amino acid as intermediate for the synthesis of chiral organic compounds.
专利号:US-9783800-B2 优先权日:2014-02-03 标 题:Method for producing peptides having azole-derived skeleton 发明人:SUGA HIROAKI; GOTO YUKI; KATO YASUHARU 权利人:UNIV TOKYO 摘要:Object of the present invention is to develop an artificial synthesis system of various peptides having an azole derivative structure and develop a library of such peptides. The present invention provides a method of producing a peptide having, in the backbone thereof, an azole derivative structure comprising the step of: synthesizing a substrate peptide of an azoline structure introducing enzyme having, in the modified region thereof, at least any one of the following amino acids, n n[in any of the compounds,n X 1 represents a group selected from the group consisting of SH, OH, NH 2 , SR 1 , OR 1 , NHR 1 , and N 3 (R 1 represents a protecting group), X 2 represents an easily eliminable group; and X 3 represents hydrogen or a substituted or unsubstituted alkyl or aryl group having from 1 to 10 carbon atoms]; reacting the substrate peptide with an azoline structure introducing enzyme to obtain a peptide having an azoline derivative structure; and converting the azoline derivative structure of the resulting peptide into an azole derivative structure by inducing an HX 2 elimination reaction of X 2 group.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.
合成参考文献
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 442. 参考文献:10.1007/bf01388170 摘要:Calmes M, Daunis J. How to build optically active alpha-amino acids. Amino Acids. 1999;16(3-4):215–50. doi: 10.1007/bf01388170.