1073371-77-3

Usage

Uses

2-Amino-5-chlorophenylboronic acid, pinacol ester

Upstream product

• 873-38-1 4-chloro-2-bromoaniline 
• 73183-34-3 bis(pinacol)diborane 
• 25015-63-8 4,4,5,5-tetramethyl-[1,3,2]-dioxaboralane 
• 106-47-8 4-chloro-aniline 

Downstream Products

• 1445865-58-6 ethyl (3S)-7-(2-amino-5-chlorophenyl)-5-oxo-1,2,3,5-tetrahydroindolizine-3-carboxylate 

Relevant academic research and scientific papers

Heterocyclic compound and application thereof

The invention discloses a heterocyclic compound and application thereof. The invention provides a heterocyclic compound shown as a formula I, a stereoisomer thereof or a pharmaceutically acceptable salt thereof. The compound can be used as an FXIa inhibit

CRYSTALLINE FORMS OF (9R, 135S)-13- {4-[5-CHLORO-2-(4-CHLORO-1H,2,3- TRIAZOL- 1 -YL)PHENYL] -6-OXO- 1,6-DIHYDROPYRIMIDIN- 1-YL}-3-(DIFLUOROMETHYL)-9-METHYL-3,4,7,15- TETRAAZATRICYCLO [ 12.3.1.02·6] OCTADECA- 1(18), 2(6), 4, 14, 16-PENTAEN-8-ONE

Disclosed are crystalline forms of Compound (I). Compound (I) is useful as an anti-thromboembolic agent in the treatment of cardiovascular diseases.

Pyridone or pyrimidinone derivatives as well as preparation method and application thereof

The present invention relates to pyridone or pyrimidinone derivatives. The invention discloses a preparation method and application thereof in medicine. , The present invention relates to a pyridone or pyrimidinone derivative represented by general formula (I), a preparation method thereof and a pharmaceutically acceptable salt thereof and as a therapeutic agent, in particular as a coagulation factor XIa (FXIa) inhibitor, wherein the definition of each substituent in the general formula (I) is the same as defined in the specification.

Oxidation of Nonactivated Anilines to Generate N-Aryl Nitrenoids

A low-temperature, protecting-group-free oxidation of 2-substituted anilines has been developed to generate an electrophilic N-aryl nitrenoid intermediate that can engage in C-NAr bond formation to construct functionalized N-heterocycles. The exposure of 2-substituted anilines to PIFA and trifluoroacetic acid or 10 mol percent Sc(OTf)3 triggers nitrenoid formation, followed by productive and selective C-NAr and C-C bond formation to yield spirocyclic- or bicyclic 3H-indoles or benzazepinones. Our experiments demonstrate the breadth of these oxidative processes, uncover underlying fundamental elements that control selectivity, and demonstrate how the distinct reactivity patterns embedded in N-aryl nitrenoid reactive intermediates can enable access to functionalized 3H-indoles or benzazepinones.

I(III)-catalyzed oxidative cyclization - Migration tandem reactions of unactivated anilines

An I(III)-catalyzed oxidative cyclization-migration tandem reaction using Selectfluor as the oxidant was developed that converts unactivated anilines into 3H-indoles is reported herein. The reaction requires as little as 1 mol % of the iodocatalyst and is mild, tolerating pyridine and thiophene functional groups, and the dependence of the diastereoselectivity of the process on the identity of the iodoarene or iodoalkane precatalyst suggests that the catalyst is present for the stereochemical determining C-N bond forming step.

Methyl-2,2-difluoro-2-(fluorosulfonyl) acetate (MDFA)/copper (I) iodide mediated and tetrabutylammonium iodide promoted trifluoromethylation of 1-aryl-4-iodo-1,2,3-triazoles

While several methods are available for the synthesis of a host of trifluoromethylated heterocycles, very few of them have been applied to access 4-trifluoromethylated 1,2,3-triazoles. We report herein a general methodology for the trifluoromethylation of 1-aryl-4-iodo-1, 2, 3-triazoles. Tetrabutylammonium iodide (TBAI) has been shown to provide enhanced conversion in these CuI-mediated reaction using methyl 2,2-difluoro-2-(fluorosulfonyl)acetate (MDFA). The method exhibited broad functional group tolerance and was applied to the synthesis of a library of 1-aryl-4-trifluoromethyl-1,2,3-triazoles on the multi-gram scale.

Alkoxy pyridone compound as well as preparation method and application thereof

The invention belongs to the field of medicinal chemistry, specifically, the invention relates to a series of inhibitors of factor XIa (FXIa for short) with a novel structure as well as a preparationmethod and an application thereof. The structure is shown as the following general formula (I). These compounds or stereoisomers, racemates, geometric isomers, tautomers, prodrugs, hydrates, solvatesor pharmaceutically acceptable salts and pharmaceutical compositions thereof can be used to treat or/and prevent related diseases mediated by factor XIa (FXIa for short).

A silicon-containing compound and comprising the silicon-containing compound of the organic electroluminescent device (by machine translation)

Provides improved emission efficiency silicon-containing compound and comprising the silicon-containing compound of the organic electroluminescent device. According to the present invention contemplates silicon-containing compound by the following formula 1 expressed. Type 1 . (by machine translation)

NOVEL SUBSTITUTED GLYCINE DERIVED FXIA INHIBITORS

The present invention provides compounds of Formula (I): [INSERT CHEMICAL STRUCTURE HERE] (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

FACTOR XIa INHIBITORS

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein.