5098-18-0

Upstream product

• 90840-73-6 benzoylamino-malonic acid diamide 
• 98-88-4 benzoyl chloride 
• 5098-14-6 2-aminomalononitrile p-toluenesulfonate 
• 5181-05-5 2-aminomalononitrile 
• 93-97-0 benzoic acid anhydride 

Downstream Products

• 34905-99-2 5-benzoylamino-2-phenyl-oxazole-4-carboxylic acid amide 
• 25680-42-6 7-Amino-2-phenyloxazolo<5,4-d>pyrimidin 
• 25680-33-5 N-(4-cyano-2-phenyl-oxazol-5-yl)-formimidic acid ethyl ester 
• 99185-68-9 5-amino-2-phenyl-oxazole-4-carboxylic acid amide 
• 958633-59-5 2-phenyl-5,6,7,8-tetrahydrooxazolo[5,4-b]quinolin-9-amine 
• 958633-62-0 2-phenyl-6,7,8,9-tetrahydro-5H-cyclohepta[b]oxazolo[4,5-e]pyridin-10-amine 
• 33360-19-9 2-phenyl-7-chloro[1,3]oxazolo[5,4-d]pyrimidine 
• 1365531-67-4 methyl 3-(4-cyano-2-phenyloxazol-5-ylamino)-3-oxopropanoate 
• 1365531-58-3 (2-phenyl-5-(1H-pyrrol-1-yl)oxazol-4-yl)methanamine 
• 1365531-56-1 2-phenyl-5-(1H-pyrrol-1-yl)-4-(1H-tetrazol-5-yl)oxazole 
• 1365531-52-7 2-phenyl-5-(1H-pyrrol-1-yl)oxazole-4-carbonitrile 

Relevant academic research and scientific papers

Synthesis and photocytotoxic activity of [1,2,3]triazolo[4,5-h][1,6]naphthyridines and [1,3]oxazolo[5,4-h][1,6]naphthyridines

[1,2,3]Triazolo[4,5-h][1,6]naphthyridines and [1,3]oxazolo[5,4-h][1,6]naphthyridines were synthesized with the aim to investigate their photocytotoxic activity. Upon irradiation, oxazolo-naphtapyridines induced light-dependent cell death at nanomolar/low

[Cu3(BTC)2]: A metal–organic framework as an environment-friendly and economically catalyst for the synthesis of tacrine analogues by Friedl?nder reaction under conventional and ultrasound irradiation

Using a green and simple route with ultrasound illumination, atmospheric pressure and room temperature, for synthesizing tacrine analogues in the presence of [Cu3(BTC)2] as an environment-friendly and economically catalyst was consid

Development of novel oxazolo[5,4-d]pyrimidines as competitive CB2 neutral antagonists based on scaffold hopping

A series of novel oxazolo[5,4-d]pyrimidines was designed via a scaffold hopping strategy and synthesized through a newly developed approach. All these compounds were evaluated for their biological activity toward CB1/CB2 cannabinoid receptors, their metabolic stability in mice liver microsomes and their cytotoxicity against several cell lines. Eight compounds have been identified as CB2 ligands with Ki values less than 1 μM. It is noteworthy that 2-(2-chlorophenyl)-5-methyl-7-(4-methylpiperazin-1-yl) oxazolo[5,4-d]pyrimidine 47 and 2-(2-chlorophenyl)-7-(4-ethylpiperazin-1-yl)- 5-methyloxazolo[5,4-d]pyrimidine 48 showed CB2 binding affinity in the nanomolar range and significant selectivity over CB1 receptors. Interestingly, functionality studies imply that they behave as competitive neutral antagonists. Moreover, all tested compounds are devoid of cytotoxicity toward several cell lines, including Chinese hamster ovary cells (CHO) and human colorectal adenocarcinoma cells HT29.

Synthesis and heterocyclization of 5-amino-4-cyano-1, 3-oxazoles

A convenient one-pot method for synthesis of some new oxazolo[5,4-d] pyrimidines via base catalyzed heterocyclization of 2-substituted 5-amino-4-cyano-1,3-oxazoles with various isothiocyanates is described.

Microwave-mediated synthesis and manipulation of a 2-substituted-5- aminooxazole-4-carbonitrile library

A 2-substituted-5-aminooxazole-4-carbonitrile library has been synthesised and modified via microwave-mediated and flow chemistries. One synthesised compound, 5-(1H-pyrrol-1-yl)-4-(1H-tetrazol-5-yl)-2-(thien-2-yl)oxazole, contains three distinct heterocyc

Synthesis and friedlaender reactions of 5-amino-4-cyano-1,3-oxazoles

The synthesis of 2-substituted 5-amino-4-cyano-l,3-oxazoles (1-4, 6-11) and the Friedaender-type reaction of compounds 1, 3, 4 is described. Compounds 13-17 are tacrine (18) analogues provided by the Friedlaender reaction. The anti-cholinesterase activity

Evolution of the thienopyridine class of inhibitors of IκB kinase-β: Part I: Hit-to-lead strategies

High-throughput screening is routinely employed as a method for the identification of novel hit structures. Large numbers of active compounds are typically procured in this way and must undergo a rigorous validation process. This process is described in detail for a collection of screening hits identified as inhibitors of IκB kinase-β (IKKβ), a key regulatory enzyme in the nuclear factor-κB (NF-κB) pathway. From these studies, a promising hit series was selected. Subsequent lead generation activities included the development of a pharmacophore hypothesis and structure-activity relationship (SAR) for the hit series. This led to the exploration of related scaffolds offering additional opportunities, and the various structural classes were comparatively evaluated for enzyme inhibition, selectivity, and drug-like properties. A novel lead series of thienopyridines was thereby established, and this series advanced into lead optimization for further development.

PREPARATION OF 2-ALKYL- AND 2-ARYL-5-AMINO-4-CYANO-1,3-OXAZOLES

Aminopropanedinitrile p-toluenesulfonate (aminomalonitrile tosylate, AMNT) reacts with acid chlorides to give 2-alkyl- and 2-aryl-5-amino-4-cyano-1,3-oxazoles in good to excellent yields.