L-焦谷氨酸置于高氯酸,碳酸氢钠体系中,用 醋酸叔丁酯 作为反应溶剂,以13.68 G (72%)的收率获得产物l-焦谷氨酸叔丁酯 参考文献:Inhibitors Of Hepatitis C Virus Ns3 Protease 标题:Inhibitors Of Hepatitis C Virus Ns3 Protease 摘要:本发明一般涉及一种新型的嘧啶酮类化合物,具有如下式(i)所示的结构,这些化合物可用作丝氨酸蛋白酶抑制剂,更具体地作为丙型肝炎病毒ns3蛋白酶抑制剂.本发明还涉及包含这些化合物的药物组合物以及使用这些药物的方法.
专利号:US-2012053350-A1 优先权日:2009-04-30 标题 :Preparation of alkyl esters of n-protected oxo-azacycloalkylcarboxylic acids 发明人:MANGION IAN; HUFFMAN MARK A; RUCK REBECCA T; LYNCH JOSEPH; CHUNG JOHN Y L; MARCUNE BENJAMIN 权利人:MANGION IAN; HUFFMAN MARK A; RUCK REBECCA T; LYNCH JOSEPH; CHUNG JOHN Y L; MARCUNE BENJAMIN 摘要:A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein P G1 is an amine protective group; k is 0, 1, or 2; and R U , R 1 , R 2 , and R 3 are defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (R U ) 3 S(O)Z, wherein Z is halide, in the presence of a strong base to obtain Compound II. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.
专利号:US-5962487-A 优先权日:1997-12-16 标题 :Antipicornaviral compounds and methods for their use and preparation 发明人:WEBBER STEPHEN E; DRAGOVICH PETER S; PRINS THOMAS J; LITTLEFIELD ETHEL S; MARAKOVITS JOSEPH T; BABINE ROBERT E 权利人:AGOURON PHARMA 摘要:Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.
专利号:CN-117510377-A 优先权日:2023-11-20 标题:Synthesis method of N alpha-fluorenylmethoxycarbonyl-glutamic acid-alpha-tert-butyl ester
参考文献:10.1016/j.tetasy.2007.02.010 摘要:Wagger J, Grdadolnik SG, Grošelj U, Meden A, Stanovnik B, Svete J. Chiral solvating properties of (S)-1-benzyl-6-methylpiperazine-2,5-dione. Tetrahedron: Asymmetry. 2007 Mar;18(4):464–75. doi: 10.1016/j.tetasy.2007.02.010.