[EN] TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C [FR] COMPOSÉS HÉTÉROCYCLIQUES TÉTRACYCLIQUES ET LEURS PROCÉDÉS D'UTILISATION POUR LE TRAITEMENT DE L'HÉPATITE C
TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C
申请人:MERCK SHARP & DOHME CORP.
公开号:US20150368246A1
公开(公告)日:2015-12-24
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
Condition-Dependent Selective Synthesis of Indolo[1,2-<i>c</i>]quinazolines and Indolo[3,2-<i>c</i>]quinolines from 2-(1<i>H</i>-Indol-2-yl)anilines and Sulfoxonium Ylides
作者:Guang Chen、Xinyuan Cai、Xinying Zhang、Xuesen Fan
DOI:10.1021/acs.joc.2c00858
日期:2022.8.5
intramolecular N– or C– nucleophilic addition and deoxygenative aromatization. This switchable synthesis was condition-dependent. In the presence of K2CO3 in CH3CN, the reaction mainly furnished indolo[1,2-c]quinazolines. In the presence of HOAc in dioxane, it selectively afforded indolo[3,2-c]quinolines. In addition, direct C–H/N–H functionalization of the products obtained provides a convenient and direct
本文介绍了通过 2-(1 H -indol-2-yl) 苯胺与氧化鎓叶立德的级联反应选择性合成吲哚[1,2- c ]喹唑啉和吲哚[3,2- c ]喹啉的方法。 . 产物的形成包括从亚砜叶立德生成卡宾物质及其与 2-(1 H-吲哚-2-基)苯胺的 N-H 键插入反应,然后形成脱氧亚胺、分子内 N- 或 C- 亲核加成和脱氧芳构化。这种可切换的合成依赖于条件。在CH 3 CN中存在 K 2 CO 3时,反应主要生成吲哚[1,2- c]喹唑啉。在二恶烷中存在 HOAc 时,它选择性地提供吲哚[3,2- c ]喹啉。此外,所得产物的直接 C-H/N-H 官能化为获得多环杂芳族化合物提供了方便和直接的途径。这些新颖的协议具有诸如易于获得的底物、易于调节的选择性、与不同官能团的良好相容性以及使用空气作为免费且可持续的氧化剂等优点。
US9493461B2
申请人:——
公开号:US9493461B2
公开(公告)日:2016-11-15
[EN] TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES TÉTRACYCLIQUES ET LEURS PROCÉDÉS D'UTILISATION POUR LE TRAITEMENT DE L'HÉPATITE C
申请人:MERCK SHARP & DOHME
公开号:WO2014121417A1
公开(公告)日:2014-08-14
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.
Palladium(II)-Catalyzed Cycloamidination via C(sp2)H Activation and Isocyanide Insertion
作者:Yong Wang、Qiang Zhu
DOI:10.1002/adsc.201200106
日期:2012.7.9
An efficient method for the synthesis of nitrogen heterocycles containing a cyclic amidine moiety has been developed. The process involves palladium‐catalyzed C(sp2)Hactivation and isocyanideinsertion starting with readily accessible ortho‐heteroarene‐substituted aniline derivatives under mild conditions.