该化合物是一种氟化β-酯化合物,通常用作有机合成的多用途中间体,其结构具有一种与一个酯功能相邻的活性基托组,对构建异性循环,药品和精细化学品很有价值;四氟苯基的存在增强了其在药用化学中的用途,特别是在将氟芳香系统引入目标分子方面.该化合物在普通有机溶剂中表现出良好的溶解性,便于其在Claisen condenations 或 Michael 附加物等反应中使用,其在标准处理条件下的稳定性和明确界定的再活动特征有助于其在合成应用中的可靠性.
4-氟苯乙酮 反应生成4-氟苯甲酰乙酸乙酯 参考文献:Heterocyclic Derivative And Medicine 标题:Heterocyclic Derivative And Medicine 摘要:一种药物组合物,包括以下通式[i]或其盐的化合物.其中r1代表芳基或杂芳基基团.R2代表氢,烷基,烯基,环烷基,环烷基烷基,羟基烷基,卤代烷基,烷氧基,烷硫基,氨基,单烷基氨基,双烷基氨基或苯基.R3和r4独立地代表氢或烷基,或r3和r4与相邻的n原子结合形成5-至7-成员的环氨基团.A代表单键的c2-10烷基.W代表o,S或(ch2)n(其中ch可以被烷基取代;N是1或2的整数).X,Y和z可以相同或不同,每个代表ch(可以被烷基取代)或n.然而,不包括x,Y和z同时代表ch的情况.该发明的化合物具有出色的神经元死亡抑制活性,并可用作治疗脑血管疾病的治疗药物.
专利号:US-4613610-A 优先权日:1984-06-22 标题 :Cholesterol biosynthesis inhibiting pyrazole analogs of mevalonolactone and its derivatives 发明人:WAREING JAMES R 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Compounds of the formula wherein R1 is C1-6alkyl not containing an asymmetric carbon atom, each of R2 and R5 is independently hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenyl, phenoxy or benzyloxy, each of R3 and R6 is independently hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, each of R4 and R7 is independently hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, with the provisos that not more than one of R2 and R3 is trifluoromethyl, not more than one of R2 and R3 is phenoxy, not more than one of R2 and R3 is benzyloxy, not more than one of R5 and R6 is trifluoromethyl, not more than one of R5 and R6 is phenoxy, and not more than one of R5 and R6 is benzyloxy, X is -(CH2)m-, -CH=CH-, -CH=CH-CH2- or -CH2-CH=CH-, wherein m is 0, 1, 2 or 3, and Z is wherein R10 is hydrogen or C1-3alkyl, wherein R12 is a physiologically acceptable and hydrolyzable ester group, and M is a pharmaceutically acceptable cation, with the provisos that (i) the-X-Z group is in the 4- or 5-position of the pyrazole ring, and (ii) the R1 group and the -X-Z group are ortho to each other, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
专利号:US-2016130259-A1 优先权日:2013-06-24 标题 :Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases 发明人:LIU HONG; DAI XING; PALANI ANANDAN; HE SHUWEN; NARGUND RAVI; XIAO DONG; DANG QUN; PENG XUANJIA; LI PENG 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula I that are useful 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-9364482-B2 优先权日:2013-06-24 标 题 :Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases 发明人:DAI XING; LIU HONG; PALANI ANANDAN; HE SHUWEN; NARGUND RAVI; XIAO DONG; ZORN NICOLAS; DANG QUN; MCCOMAS CASEY C; PENG XUANJIA; LI PENG; SOLL RICHARD 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula I that are useful 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. (I)
专利号:US-9265773-B2 优先权日:2011-09-08 标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases 发明人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; HE SHUWEN; DAI XING; LIU HONG; LAI ZHONG; LONDON CLARE; XIAO DONG; ZORN NICOLAS; NARGUND RAVI 权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; HE SHUWEN; DAI XING; LIU HONG; LAI ZHONG; LONDON CLARE; XIAO DONG; ZORN NICOLAS; NARGUND RAVI; MERCK SHARP & DOHME; MSD ITALIA SRL 摘要:The present invention relates to compounds of formula (I) that are useful 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-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-9549917-B2 优先权日:2011-09-08 标 题 :Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases 发明人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; LAI ZHONG; DANG QUN; ZORN NICOLAS 权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; LAI ZHONG; DANG QUN; ZORN NICOLAS; MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful 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.
参考标题:Glutamate As An Efficient Amine Donor For The Synthesis Of Chiral β‐ And γ‐amino Acids Using Transaminase 作者:Geon‐hee Kim,Hyunwoo Jeon,Taresh P. Khobragade,Mahesh D. Patil,Sihyong Sung,Sanghan Yoon,Yumi Won,Sharad Sarak,Hyungdon Yun |发布日期:2019.3.6 摘要:A Recyclable Glutamate Amine Donor System Employing Transaminase (Ta), Glutamate Dehydrogenase (Gludh) And Mutant Formate Dehydrogenase (Fdhm) Was Developed, Wherein Amine Donor Glu Was Regenerated Using Gludh And Thereby Circumvented The Inhibition Of Ta By α‐ketoglutarate. Various Enantiopure β‐, γ‐amino Acids, And Amines Were Successfully Synthesized With High Conversions And Excellent Enantiomeric
合成参考文献
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