54998-29-7

Upstream product

• 3717-21-3 p-methoxyl benzaldoxime 
• 874-90-8 4-methoxybenzonitrile 
• 75-36-5 acetyl chloride 
• 123-11-5 4-methoxy-benzaldehyde 
• 64-17-5 ethanol 

Downstream Products

• 1014-25-1 5-(4-methoxy-phenyl)-[1,3,4]thiadiazol-2-ylamine 
• 96134-01-9 4-methoxy-N'-thiocarbamoyl-benzohydrazonic acid ethyl ester 
• 66842-88-4 N-(2-diethylamino-ethyl)-4-methoxy-benzamidine 
• 2564-57-0 4-carbomethoxy-2-(4-methoxyphenyl)-δ²-thiazoline 
• 51721-68-7 4-methoxybenzamidine hydrochloride 
• 33901-36-9 5-(4-methoxyphenyl)-2,4-dihydro-3H[1,2,4]triazole-3-thione 
• 91759-68-1 5-(4-methoxyphenyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione 
• 96424-91-8 2-[3-(4-Methoxy-phenyl)-5-methylsulfanyl-[1,2,4]triazol-4-yl]-ethanol 
• 96134-09-7 4-(2-Hydroxy-ethyl)-5-(4-methoxy-phenyl)-2,4-dihydro-[1,2,4]triazole-3-thione 
• 23282-98-6 4-benzyl-5-(4-methoxyphenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione 
• 96134-15-5 5-(4-Methoxy-phenyl)-4-phenylamino-2,4-dihydro-[1,2,4]triazole-3-thione 
• 96134-47-3 [3-(4-Methoxy-phenyl)-5-methylsulfanyl-[1,2,4]triazol-4-yl]-phenyl-amine 
• 96134-21-3 N-[3-(4-Methoxy-phenyl)-5-thioxo-1,5-dihydro-[1,2,4]triazol-4-yl]-benzamide 
• 1103883-35-7 ethyl (S)-2-(4-methoxyphenyl)-4,5-dihydrooxazole-4-carboxylate 

Relevant academic research and scientific papers

Microwave-assisted synthesis of new 2-aryl and 2-alkylimidazolones and evaluation of their in vitro anticancer activity and their in vivo toxicity on zebrafish embryos

Herein we describe the synthesis of five new 2-aryl and 2-alkylimidazolone derivatives via an effective one-pot synthetic strategy assisted by microwave irradiations which allowed us to access the desired product in a reduced time reaction compared to the

DNA-Encoded Libraries: Hydrazide as a Pluripotent Precursor for On-DNA Synthesis of Various Azole Derivatives

DNA-encoded combinatorial chemical library (DEL) technology, an approach that combines the power of genetics and chemistry, has emerged as an invaluable tool in drug discovery. Skeletal diversity plays a fundamental importance in DEL applications, and relies heavily on novel DNA-compatible chemical reactions. We report herein a phylogenic chemical transformation strategy using DNA-conjugated benzoyl hydrazine as a common versatile precursor in azole chemical expansion of DELs. DNA-compatible reactions deriving from the common benzoyl hydrazine precursor showed excellent functional group tolerance with exceptional efficiency in the synthesis of various azoles, including oxadiazoles, thiadiazoles, and triazoles, under mild reaction conditions. The phylogenic chemical transformation strategy provides DELs a facile way to expand into various unique chemical spaces with privileged scaffolds and pharmacophores.

Colchicine derivatives, and preparation method and medical application thereof

The invention specifically relates to colchicine derivatives (I) as described in the specification and a preparation method thereof, and pharmaceutical compositions containing the colchicine derivatives, belonging to the field of medicinal chemistry. The results of pharmacodynamic experiments prove that the colchicine derivatives of the invention have treatment effect on lumbar disc herniation andliver fibrosis.

Fluorescent benzene-centered mono-, bis- and tris-triazapentadiene-boron complexes

A series of novel benzene centered mono-, bis- and tris-1,3,5-triazapentadiene ligands 6a-e was synthesized and investigated with respect to their reactivity towards triphenylborane. The resulting blue-fluorescent boron complexes 14a-e with a six-membered

Facile synthesis of 3,5-diaryl-1,2,4-triazoles via copper-catalyzed domino nucleophilic substitution/oxidative cyclization using amidines or imidates as substrates

Two methods for the synthesis of 3,5-diaryl-1,2,4-triazoles, both domino reactions, are reported. The first procedure, the Cu(OTf)2-catalyzed reaction between two amidines using NaHCO3 as a base, 1,10-phenanthroline as an additive and K3[Fe(CN)6]/ atmospheric oxygen as the oxidant, delivers 3,5-diaryl-1,2,4-triazoles with yields up to 68%. The second procedure for the synthesis of 3,5-diaryl-1,2,4- triazoles with yields up to 64% rests on the Cu(OTf)2-catalyzed reaction between two imidates and ammonium carbonate. This method features the formation of three bonds in a single synthetic step.

Enantioselective synthesis of α-benzylated lanthionines and related tripeptides for biological incorporation into E. coli peptidoglycan

The synthesis of modified tripeptides (S)-Ala-γ-(R)-Glu-X, where X = (R,S) or (R,R) diastereomers of α-benzyl or α-(4-azidobenzyl)lanthionine, was carried out. The chemical strategy involved the enantioselective alkylation of a 4-MeO-phenyloxazoline. The reductive opening of the alkylated oxazolines, followed by cyclization and oxidation, led to four PMB-protected sulfamidates. Subsequent PMB removal, Boc protection and regioselective opening with cysteine methyl ester led to protected lanthionines. These compounds were further converted in a one pot process to the corresponding protected tripeptides. After ester and Boc deprotection, the four tripeptides were evaluated as potential analogues of the natural tripeptide (S)-Ala-γ-(R)-Glu-meso-A2pm. These compounds were evaluated for introduction, by means of the biosynthetic recycling pathway, into the peptidoglycan of Escherichia coli. A successful in vitro biosynthesis of UDP-MurNAc-tripeptides from the tripeptides containing α-benzyl lanthionine was achieved using purified murein peptide ligase (Mpl). Bioincorporation into E. coli W7 did not occur under different tested conditions probably due to the bulky benzyl group at the Cα carbon of the C-terminal amino acid. This journal is

Pd(ii)-catalyzed direct C5-arylation of azole-4-carboxylates through double C-H bond cleavage

The first palladium-catalyzed direct C5-arylation of azole-4-carboxylates with simple unactivated arenes through double C-H bond cleavage is realized. This protocol provided a straightforward access to diverse 5-arylsubstituted azole-4-carboxylic derivatives with good functional group tolerance. The Royal Society of Chemistry 2012.

2-Phenyl-1-[4-(2-piperidine-1-yl-ethoxy)benzyl]-1H-benzimidazoles as ligands for the estrogen receptor: Synthesis and pharmacological evaluation

2-Phenyl-1H-benzimidazoles 7a-e were synthesized and tested for gene activation on ERα-positive MCF-7 breast cancer cells, stably transfected with the reporter plasmid EREwtcluc (MCF-7-2a cells). None of the compounds showed agonistic properties, but they antagonized dependent on hydroxyl groups at the benzimidazole core (5- or 6-OH) and at the aromatic ring in the 2-position (4-OH) in high concentrations the gene activation induced by estradiol (E2, 1 nM). All compounds exhibited significant antiproliferative properties on MCF-7 cells but they were inactive against hormone independent, ER negative MDA-MB-231 cells.

Reverse-benzamidine antimalarial agents: Design, synthesis, and biological evaluation

In the frame of the development of bis-cationic choline analogs, the RSA of bis-N-alkylamidines were studied and a new series of reverse-benzamidine derivatives was designed. Contrary to the lipophilicity, the basicity of alkylamidine compounds directly influences their antimalarial potencies.

Synthesis, structures of some unsymmetrical 3,6-disubstituted-1,2,4,5- tetrazines

(Chemical Equation Presented) A series of new unsymmetrical 3-phenyl-6-benzyl-1,2,4,5-tetrazine derivatives 10a-i were synthesized and characterized by IR, NMR, MS, and element analysis. The structures of 4a, 10c, 10d and 10h were analyzed by X-ray crystallography, which had intermolecular C-H...N, C-H...Cl, C-H...Π and Π...Π H interactions.