专利号:US-2023399302-A1 优先权日:2020-10-29 标题:Process for the preparation of heteroaryl-substituted sulfur(vi) compounds 发明人:LOPCHUK JUSTIN M; SHULTZ ZACHARY P; SCATTOLIN THOMAS 权利人:H LEE MOFFITT CANCER CT & RES 摘要:The present disclosure provides processes for the synthesis of organic compounds, in particular processes for the synthesis of heteroaryl-substituted sulfur(VI) compounds by nucleophilic aromatic substitution.
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-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.
专利号:UA-106972-C2 优先权日:2009-06-22 标题 :METHOD FOR SYNTHESIS OF DIARYL-PYRIMIDINE NON-NUCLEOSIDE INHIBITOR OF REVERSE TRANSCRIPTASIA
专利号:JP-2012509314-A 优先权日:2009-06-22 标 题:Method for the synthesis of diarylpyrimidine non-nucleoside reverse transcriptase inhibitors
专利号:WO-0116162-A1 优先权日:1999-08-28 标 题 :Method for producing cyclic peptidomimetics 发明人:SCHARN DIRK; GERMEROTH LOTHAR; WENSCHUH HOLGER 权利人:CHEMOTOPIX GMBH; SCHARN DIRK; GERMEROTH LOTHAR; WENSCHUH HOLGER 摘要:The invention relates to a method for the synthesis of cyclic peptides or peptidomimetics by means of sequential nucleophile substitutions on polyhalogenated aromatics. The method comprises the following steps: (i) A linear peptide or peptidomimetic with a free nucleophile functionality is reacted with the aromatic in the sense of a simple nucleophile aromatic substitution, whereby the nucleophile functionality is an alcohol, thiol or amine. (ii) The protective group of an additional nucleophile functionality is selectively split at the same peptide or peptidomimetic, whereby the released nucleophile functionality is an alcohol, thiol or amine and (iii) cyclisation is carried out by adding a tertiary amine or another base, whereby cyclisation is carried out by means of nucleophile aromatic substitution of an additional halogen atom of the halogen aromatic by the released nucleophile functionality, said halogen aromatic being bound to the peptide.