64310-35-6

Upstream product

• 33901-36-9 5-(4-methoxy-phenyl)-1,2-dihydro-[1,2,4]triazole-3-thione 
• 16778-84-0 4-methoxybenzoyl isothiocyanate 
• 100-07-2 4-methoxy-benzoyl chloride 
• 833-84-1 1-(4-methoxy-benzoyl)-thiosemicarbazide 
• 54682-95-0 N-(1,2,2,2-tetrachloroethyl)-4-methoxybenzimidoyl chloride 
• 63499-61-6 N-(2,2,2-trichloro-1-hydroxyethyl)-4-methoxybenzamide 
• 3424-93-9 4-methoxyphenylacetamide 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 
• 64781-78-8 3-diazo-3H-[1,2,4]triazole 
• 100-66-3 methoxybenzene 
• 54926-13-5 N-[1-Dimethylamino-meth-(E)-ylidene]-4-methoxy-benzamide 

Relevant academic research and scientific papers

VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF

Disclosed herein are small molecule Vascular Adhesion Protein- 1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.

Liganding Functional Tyrosine Sites on Proteins Using Sulfur-Triazole Exchange Chemistry

Tuning reactivity of sulfur electrophiles is key for advancing click chemistry and chemical probe discovery. To date, activation of the sulfur electrophile for protein modification has been ascribed principally to stabilization of a fluoride leaving group (LG) in covalent reactions of sulfonyl fluorides and arylfluorosulfates. We recently introduced sulfur-triazole exchange (SuTEx) chemistry to demonstrate the triazole as an effective LG for activating nucleophilic substitution reactions on tyrosine sites of proteins. Here, we probed tunability of SuTEx for fragment-based ligand discovery by modifying the adduct group (AG) and LG with functional groups of differing electron-donating and -withdrawing properties. We discovered the sulfur electrophile is highly sensitive to the position of modification (AG versus LG), which enabled both coarse and fine adjustments in solution and proteome activity. We applied these reactivity principles to identify a large fraction of tyrosine sites (～30%) on proteins (～44%) that can be liganded across >1500 probe-modified sites quantified by chemical proteomics. Our proteomic studies identified noncatalytic tyrosine and phosphotyrosine sites that can be liganded by SuTEx fragments with site specificity in lysates and live cells to disrupt protein function. Collectively, we describe SuTEx as a versatile covalent chemistry with broad applications for chemical proteomics and protein ligand discovery.

PESTICIDAL COMPOSITIONS AND METHODS

This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules,

Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity

A series of novel tetrahydropyrazolopyridone derivatives containing 1,3,4-triazole, triazolylmethyl, and partially saturated heterocyclic moieties as P2 binding element was designed, synthesized, and evaluated in vitro for anticoagulant activity in human and rabbit plasma. All compounds showed moderate to significant potency, and compounds 15b, 15c, 20b, 20c, and 22b were further examined for their inhibitory activity against human FXa in vitro. While compounds 15c and 22b were tested for rat venous thrombosis in vivo. The most promising compound 15c, with an IC50 (FXa) value of 0.14?μM and 98% inhibition rate, warranted further investigation as an FXa inhibitor.

A new, high-yield synthesis of 3-aryl-1,2,4-triazoles

A convenient new synthetic approach to 3-aryl-1,2,4-triazoles has been developed. Chloralamides were obtained by high yield reactions between benzamides and chloral hydrate. These reacted with a phosphorus pentachloride/phosphorus oxychloride mixture unde

SUBSTITUENT AND COORDINATION EFFECTS IN SINGLET REACTIONS OF 3-DIAZO-3H-1,2,4-TRIAZOLES WITH SUBSTITUTED BENZENES AND NITRO COMPOUNDS

3-Diazo-3H-1,2,4-triazoles convert to singlet 3H-1,2,4-triazol-3-ylidenes which (1) effect directed electrophilic substitutions of benzenes and (2) coordinate with benzenoid substituents and nitro compounds to give decomposition or rearrangement products.

About Nitrile-Formamide-Chloride-Adducts. IX - Synthesis of 1,3- or 1,5-Disubstituted 1,2,4-Triazoles by the Reaction of Nitrile-Formamide Chloride-Adducts and their Products of Hydrolysis with Hydrazines

2-Aza-3-chloro-2-propeniminium salts 5, which are easily available by the addition of formamide chlorides 1 to nitriles 2 react smoothly with hydrazines 9 giving rise to 1,3-disubstituted 1,2,4-triazoles 11.When the 2-aza-3-chloro-2-propeniminium salts 5