1420069-56-2

Upstream product

• 98-59-9 p-toluenesulfonyl chloride 
• 100846-24-0 5-trifluoromethyl-1H-indole 
• 6146-52-7 5-nitroindole 
• 107491-54-3 4-methyl-N-(4-trifluoromethyl-phenyl)-benzenesulfonamide 
• 1186610-43-4 N-(2-ethynyl-4-(trifluoromethyl)phenyl)-4-methylbenzenesulfonamide 

Downstream Products

• 1420069-57-3 [1-[(4-methylphenyl)sulfonyl]-5-(trifluoromethyl)-1H-indol-3-yl]boronic acid 
• 1420069-58-4 N-ethyl-N-({2-[1-[(4-methylphenyl)sulfonyl]-5-(trifluoromethyl)-1H-indol-3-yl]pyridin-3-yl}methyl)cyclopropanecarboxamide 

Relevant academic research and scientific papers

Facile synthesis of indoles by K2CO3catalyzed cyclization reaction of 2-ethynylanilines in water

The cyclization reaction of 2-ethynyl-N-sulfonylanilides proceeded efficiently in water with the presence of a catalytic amount of K2CO3under transition metal-free condition to give indoles in high yields. The recovery and reusabilit

A Catalytic Construction of Indoles via Formation of Ruthenium Vinylidene Species from N-Arylynamides

Treatment of ynamides with a catalytic amount of TpRuCl(PPh3)2 resulted in the construction of indole scaffolds known as privileged structure motifs. This reaction involved a cascade of 1,2-rearrangement and cyclization carrying out C?C bond formation via a ruthenium vinylidene intermediate, as revealed by a deuterium-labeling experiments. Furthermore, the transformation of multi-functionalized ynamide, derived from a practical drug molecule, showed a high functional group tolerance of this reaction. (Figure presented.).

Iodine-Mediated Electrochemical C(sp2)-H Amination: Switchable Synthesis of Indolines and Indoles

A metal-free electrochemical intramolecular C(sp2)-H amination using iodine as a mediator was developed. This method enables a switchable synthesis of indoline and indole derivatives, respectively, from easily available 2-vinyl anilines.

SUBSTITUTED INDOLE DERIVATIVES AS DENGUE VIRAL REPLICATION INHIBITORS

The present invention concerns substituted indole derivatives, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent

INDOLE DERIVATIVES AS DENGUE VIRAL REPLICATION INHIBITORS

The present invention relates to mono- or di-substituted indole compounds, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat

MONO- OR DI-SUBSTITUTED INDOLE DERIVATIVES AS DENGUE VIRAL REPLICATION INHIBITORS

The present invention relates to mono- or di-substituted indole compounds, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.

Conversion of aromatic amino into trifluoromethyl groups through a Sandmeyer-type transformation

A novel strategy for aromatic trifluoromethylation by converting amino into trifluoromethyl groups via a Sandmeyer-type reaction is reported. The transformation involves diazotization of the aromatic amines with tert-butyl nitrite and hydrochloric acid to form aryldiazonium chlorides, followed by trifluoromethylation with trifluoromethylsilver at low temperature. Various readily available aromatic amines are smoothly converted under mild conditions. Georg Thieme Verlag Stuttgart. New York.

Silver-mediated trifluoromethylation of aryldiazonium salts: Conversion of amino group into trifluoromethyl group

A novel strategy for aromatic trifluoromethylation by converting aromatic amino group into CF3 group is reported herein. This method, which can be considered as trifluoromethylation variation of the classic Sandmeyer reaction, uses readily available aromatic amines as starting materials and is performed under mild conditions.

New CRTh2 antagonists.

The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.

NEW CRTh2 ANTAGONISTS

The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.