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5-溴-2-氯吡啶置于n1,N2-双(2-噻吩甲基)-乙二酰胺,Caesium Carbonate,Copper(I) Bromide,Sodium Hydroxide体系中,用 水,二甲基亚砜 作为反应溶剂,化学反应 20.0H,以56%的收率获得产物2-氯-5-羟基吡啶
参考文献:从药物化合物库中鉴定铜催化的c-O偶联的草酰胺配体
标题:从药物化合物库中鉴定铜催化的c-O偶联的草酰胺配体
摘要:一个典型的药物化合物库具有分子多样性,可以为发现新的配体结构提供平台.本文中,我们描述了这种方法与高通量筛选的结合使用,以鉴定n,N'-双(噻吩-2-基甲基)草酰胺为配体,通常对铜催化的c-O交叉偶联有效.在温和的条件下都可以同时使用联芳醚和苯酚.
DOI:10.1002/cctc.201900393

专利信息

专利号:US-9242998-B2
优先权日:2013-02-07
标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
发明人：HE SHUWEN; DAI XING; PALANI ANANDAN; NARGUND RAVI; LAI ZHONG; ZORN NICOLAS; XIAO DONG; DANG QUN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD
权利人:HE SHUWEN; DAI XING; PALANI ANANDAN; NARGUND RAVI; LAI ZHONG; ZORN NICOLAS; XIAO DONG; DANG QUN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD; 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-9243002-B2
优先权日:2013-02-07
标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
发明人：DAI XING; LIU HONG; PALANI ANANDAN; HE SHUWEN; BROCKUNIER LINDA L; NARGUND RAVI; MARCANTONIO KAREN; ZORN NICOLAS; XIAO DONG; PENG XUANJIA; LI PENG; GUO TAO
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-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-2007275968-A1
优先权日:2004-09-07
标 题 :Substituted Biphenyl Derivative
发明人：KURATA HITOSHI; NISHIMATA TOYOKI; WATANABE YUKIKO; EBISAWA MASAYUKI; FUJIMOTO TEPPEI; KOBAYASHI HIDEKI
权利人:KURATA HITOSHI; NISHIMATA TOYOKI; WATANABE YUKIKO; EBISAWA MASAYUKI; FUJIMOTO TEPPEI; KOBAYASHI HIDEKI
摘要:The present invention relates to a biaryl derivative or a pharmacologically acceptable salt thereof having an excellent collagen-synthesis inhibition activity. A biaryl derivative having a structure represented by the following General Formula (I) or a pharmacologically acceptable salt thereof: n nwherein n R 1 represents a C 6 -C 10 aryl group which is substituted with one to three group(s) each independently selected from the group consisting of a group defined by formula R-L-, a di-(C 1 -C 6 alkyl)amino group, a di-(C 1 -C 6 alkyl)aminosulfonyl group, a hydroxyaminocarbonyl group, and a halogen atom, and so on; R represents a C 1 -C 6 alkyl group, and so on; L represents a sulfonyl group, an aminosulfonyl group, or a sulfonylamino group, and so on; R 2 represents a hydrogen atom, and so on; A represents a group defined by formula (II), (III), or (IV); R 3 represents a C 1 -C 6 alkyl group, and so on; and R 4 represents a C 1 -C 6 alkyl group, and so on.