85862-71-1

Upstream product

• 288-36-8 1,2,3-triazole 
• 1194-02-1 4-fluorobenzonitrile 
• 873-74-5 4-Aminobenzonitrile 
• 619-72-7 4-nitrobenzonitrile 
• 18523-41-6 4-azidobenzonitrile 
• 1066-54-2 trimethylsilylacetylene 
• 623-00-7 4-bromobenzenecarbonitrile 

Downstream Products

• 1616598-39-0 (4-(1H-1,2,3-triazol-1-yl)phenyl)methanamine 
• 1616598-41-4 N-(4-(1H-1,2,3-triazol-1-yl)benzyl)-2-chloro-5-methylpyrimidin-4-amine 
• 1616598-33-4 N-(4-(1H-1,2,3-triazol-1-yl)benzyl)-5-methyl-2-(2-isopropylphenyl)pyrimidin-4-amine trifluoroacetic acid 
• 1364524-44-6 4-(1H-4,2,3-triazolyl-1-yl)benzoyl chloride 

Relevant academic research and scientific papers

[4 + 1] Annulation of in situ generated azoalkenes with amines: A powerful approach to access 1-substituted 1,2,3-triazoles

1-Substituted 1,2,3-triazoles represents ‘privileged’ structural scaffolds of many clinical pharmaceuticals. However, the traditional methods for their preparation mainly rely on thermal [3 + 2] cycloaddition of potentially dangerous acetylene and azides. Here we report a base-mediated [4 + 1] annulation of azoalkenes generated in situ from readily available difluoroacetaldehyde N-tosylhydrazones (DFHZ-Ts) with amines under relatively mild conditions. This azide- and acetylene-free strategy provides facile access to diverse 1-substituted 1,2,3-triazole derivatives in high yield in a regiospecific manner. This transformation has great functional group tolerance and can suit a broad substrate scope. Furthermore, the application of this novel methodology in the gram-scale synthesis of an antibiotic drug PH-027 and in the late-stage derivatization of several bioactive small molecules and clinical drugs demonstrated its generality, practicability and applicability.

A post-synthetically modified metal-organic framework for copper catalyzed denitrative C-N coupling of nitroarenes under heterogeneous conditions

Here we report, for the first time, the Ullmann C-N coupling reaction of nitroarenes which is achieved by using a copper containing metal-organic framework (MOF) catalyst under heterogenous conditions. The ready availability of nitroarenes and their low cost have made them ideal replacements for haloarenes as electrophilic coupling partners. Notably, the reaction protocol suppresses the by-product formation in the catalytic reaction. The catalyst has been designed and synthesized by two step post-synthesis functionalization of a MOF,viz.dabco MOF-1 with a -NH2functional group (DMOF-NH2). In the post-synthetic treatment, salicylaldehyde has been used for organic modification first and then copper(ii) was successfully incorporated onto the inner surface of the porous material. The hybrid porous solid thus obtained has been employed in the catalytic C-N coupling reaction of nitroarenes with a wide variety of amines under heterogeneous conditions, which displayed very high turnover frequencies (TOF) in catalytic reactions attesting its efficacy towards theN-arylation reaction.

PURINONES AS UBIQUITIN-SPECIFIC PROTEASE 1 INHIBITORS

The application relates to inhibitors of USP1 useful in the treatment of cancers, and other USP1 associated diseases and disorders, having the Formula: (I), where R1, R2, R3, R3', R4, R5, X1, X2, X3, X4, and n are described herein.

KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE

Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

INHIBITORS OF THE USP1/UAF1 DEUBIQUITINASE COMPLEX AND USES THEREOF

Disclosed are inhibitors of the USP1/UAF1 deubiquitinase complex, for example. of formula (I), wherein R1, R2, and Q are as defined herein, which are useful in treating diseases such as cancer, and improving the efficacy of DNA damag

2-PYRAZINONE DERIVATIVES FOR THE TREATMENT OF DISEASE OR CONDITION IN WHICH INHIBITION OF NEUTROPHIL ELASTASE ACTIVITY IS BENEFICIAL.

The invention provides compounds of formula (I) wherein R1, R3, R4, R5, R14, X and W are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acce

2-PYRIDONE DERIVATIVES FOR THE TREATMENT OF DISEASE OR CONDITION IN WHICH INHIBITION OF NEUTROPHIL ELASTASE ACTIVITY IS BENEFICIAL.

The invention provides compounds of formula (1) wherein R1, R3, R4, R5, R6, R14, X and W are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharma

1,6 - SUBSTITUTED (3R,6R) -3- (2,3-DIHYDRO-1H-INDEN-2-YL)-2,5-PIPERAZINEDIONE DERIVATIVES AS OXYTOCIN RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PRE-TERM LABOUR, DYSMENORRHEA AND ENDOMETRIOSIS

The present invention relates to compound S of Formula (I).