85862-90-4

Upstream product

• 108-05-4 vinyl acetate 
• 20062-24-2 4-azidoacetophenone 
• 403-42-9 1-(4-fluorophenyl)ethanone 
• 288-36-8 1 ,2,3-Triazole 
• 99-92-3 p-aminobenzophenone 
• 288-36-8 1,2,3-triazole 
• 99-90-1 para-bromoacetophenone 

Downstream Products

• 128864-42-6 2-Bromo-1-(4-[1,2,3]triazol-1-yl-phenyl)-ethanone 
• 128864-44-8 1-(p-dibromoacetyl-phenyl)-1H-1,2,3-triazole 
• 128864-38-0 di-<-carbonylmethylen> disulfide 

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.

An azide and acetylene free synthesis of 1-substituted 1,2,3-triazoles

This paper details a simple and efficient 3-component synthesis of 1-substituted 1,2,3-triazoles using a primary amine, 2,2-dimethoxyacetaldehyde and tosylhydrazide. The reaction proceeds in good to excellent yields using either aliphatic or aromatic amine substrates and is tolerant of a wide range of functional groups including electron-rich and deficient aryl groups, terminal alkynes, ketones and highly sterically encumbered amines.

Single-component small-molecule white light organic phosphors

White light emission from single-component small organic triazole molecules in the solid state was observed for the first time. This unusual intrinsic broadband emission, stemming from the supramolecular aggregate instead of the excimer, can be tuned by c

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.

Synthesis and antifungal activity of novel thiazole-containing triazole antifungals. II. Optically active ER-30346 and its derivatives

A series of novel thiazole-containing triazole antifungals was synthesized and evaluated for antifungal activity against a variety of clinically isolated pathogenic fungi in vitro and against systemic candidosis in vivo. These compounds showed potent antifungal activities in vitro and in vivo. In particular, (2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4- difluorophenyl)-1-(1H-1,2,4-triazol-l-yl)-2-butanol (12g; ER-30346) showed potent and well-balanced in vitro activities and potent in vivo efficacy, and had a good safety profile.

Superoxide dismutase-like activity of 1,2,3-triazole derivatives.

This paper reports the synthesis of some sulfurated 1,2,3-triazole derivatives and the biological evaluation, for the superoxide dismutase-like activity, of these new compounds together with several 1,2,3-triazoles previously described by us. All the compounds possess a SOD-like activity and some of them showed an activity equivalent to or higher than those of penicillamine or thiopronin, which are well known therapeutic drugs in the treatment of rheumatoid arthritis.