1450-76-6

Usage

Uses

Used in Pharmaceutical Industry:
2'-HYDROXY-5'-NITROACETOPHENONE is used as a potential inhibitor of platelet aggregation for the prevention and treatment of blood clot-related disorders. Its ability to inhibit platelet aggregation makes it a promising candidate for the development of anti-thrombotic drugs, which can help in reducing the risk of heart attacks, strokes, and other cardiovascular diseases.

InChI:InChI=1/C8H7NO4/c1-5(10)7-4-6(9(12)13)2-3-8(7)11/h2-4,11H,1H3/p-1

Upstream product

• 100-02-7 4-nitro-phenol 
• 108-24-7 acetic anhydride 
• 118-93-4 o-hydroxyacetophenone 
• 75-36-5 acetyl chloride 
• 14150-94-8 3,5-dinitro-1-methyl-2-pyridone 
• 15435-71-9 sodium acetylacetonate 
• 64-19-7 acetic acid 
• 61941-46-6 1-(2-methoxy-5-nitro-phenyl)-ethanone 
• 75-30-9 2-iodo-propane 
• 189814-42-4 2-isopropoxy-5-nitroacetophenone 
• 491-38-3 1-benzopyran-4(4H)-one 
• 100-17-4 para-methoxynitrobenzene 
• 123-54-6 acetylacetone 
• 14080-32-1 5-nitropyrimidine 

Downstream Products

• 3316-09-4 1,2-dihydroxy-4-nitrobenzene 
• 35234-45-8 (E)-1-(2-hydroxy-5-nitrophenyl)-3-phenylprop-2-en-1-one 
• 1776-26-7 2'-hydroxy-4-methoxy-5'-nitro-trans-chalcone 
• 111439-48-6 3-benzoyl-6-nitro-2-phenyl-chromen-4-one 
• 118761-30-1 1-(2-hydroxy-5-nitrophenyl)-3-(3-thienyl)-2-propen-1-one 
• 87699-35-2 1-(2-{2-[Bis-(2-chloro-ethyl)-amino]-ethoxy}-5-nitro-phenyl)-ethanone; hydrochloride 
• 87699-37-4 1-(2-{2-[[2-(2-Acetyl-4-nitro-phenoxy)-ethyl]-(2-chloro-ethyl)-amino]-ethoxy}-5-nitro-phenyl)-ethanone; hydrochloride 
• 97481-55-5 6-Amino-5-[1-(2-hydroxy-5-nitro-phenyl)-eth-(E)-ylideneamino]-1,3-dimethyl-1H-pyrimidine-2,4-dione 
• 50-80-6 5-amino-2-hydroxyacetophenone 
• 149744-62-7 (E)-3-(3,4-Dihydro-2H-benzo[b][1,4]dioxepin-7-yl)-1-(2-hydroxy-5-nitro-phenyl)-propenone 
• 170807-45-1 (E)-3-(6-Chloro-4H-benzo[1,3]dioxin-8-yl)-1-(2-hydroxy-5-nitro-phenyl)-propenone 
• 61941-46-6 1-(2-methoxy-5-nitro-phenyl)-ethanone 
• 508210-80-8 1-[2-(benzhydryloxy)-5-nitrophenyl]ethanone 

Relevant academic research and scientific papers

A new and improved process for celiprolol hydrochloride

Celiprolol hydrochloride, a β-blocker drug, has been synthesized by a new approach. How this new process offers distinctive advantages over the existing one will be described.

Design, synthesis and biological evaluation of novel benzopyran sulfonamide derivatives as 5-HT6 receptor ligands

On the basis of a known pharmacophore model for 5-HT6 receptor antagonists (5-HT6R), we have designed and synthesized a novel series of benzopyran sulfonamide derivatives 9(a-d), 20(a-d) and 21(a-d) and their structures were confirmed by 1H NMR and mass spectral data. All the synthesized compounds were tested for their antagonistic activity towards 5-HT6R in a cell based reporter gene in vitro functional assay. Most of the tested compounds showed moderate to potent binding affinities towards 5-HT6R.

Sigma Complexes in the Pyrimidine Series. 6. Reaction of 5-Nitro-2-methoxy- and 5-Nitro-4,6-dimethoxypyrimidines with the Acetylacetone Carbanion

Depending on the reaction conditions, the reaction of 5-nitro-2-methoxy- and 5-nitro-4,6-dimethoxypyrimidines with acetylacetone carbanion gives potassium salts of 5-nitrodiacetylmethylenepyrimidines or, as a result of recyclization of the pyrimidine ring, 5-nitro-2-hydroxyacetophenone.

Raf kinase inhibitor based on chromone structure, and preparation method and uses thereof

The invention relates to the technical field of pharmaceutical chemistry, and more concretely relates to a group of chromone compounds (A), wherein R1-R10, X1 and X2 are defined in the description. The invention also discloses a preparation method of the

A kind of two-thiazoline ketone compounds and pharmaceutical compositions thereof and use thereof (by machine translation)

The invention provides general formula (I) indicated by the thiazoline ketone compounds and pharmaceutical compositions thereof and use thereof. The compounds can be combined with the bromodomain domain of the protein, thereby adjusting the downstream signal path, to play a particular function, can be used for treating the relevant domain protein in the bromodomain of various diseases. Such compounds can be interference has Brd4 bromodomain domain with the acetylated histone binding, and then lower the oncogene c - the ventilating cabins and its related target gene transcription, so that it may be effective for treating the tumor. (by machine translation)

8-nitro-2-four azolyl-4- carbonyl benzene benzopyran synthetic method

The invention relates to a synthesis method of 8-nitro-2-tetrazol-5-yl-4-oxo-4H-1-benzopyran. The method comprises the following steps: firstly nitrifying hydroxyacetophenone taken as a starting material with a nitric acid so as to generate a mixture of 2

Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors

Two series of thienopyrimidine derivatives (10a-k, 16a-j) bearing chromone moiety were designed and synthesized. All the compounds were evaluated for inhibitory activity against mTOR kinase at a concentration of 10uM. Four selected compounds were further evaluated for the IC50 values against mTOR kinase, PI3Kα kinase and two cancer cell lines. Some of the target compounds exhibited moderate to excellent mTOR/PI3Kα kinase inhibitory activity and cytotoxicity. The most promising compound 16i showed good inhibitory activity against mTOR/PI3Kα kinase and good antitumor potency for H460 and PC-3 cell lines with IC50 values of 0.16 ± 0.03 μM, 2.35 ± 0.19 μM, 1.20 ± 0.23 μM and 0.85 ± 0.04 μM, which were 8.6, >5, 7.9 and 19.1 times more active than compound I (1.37 ± 0.07 μM, >10 μM, 9.52 ± 0.29 μM, 16.27 ± 0.54 μM), respectively. Structure-activity relationships (SARs) and docking studies indicated that the chromone moiety is necessary for the potent antitumor activity and cytotoxicity of these compounds. Substitution of the chromone moiety at the 6-position has a significant impact to the inhibitory activity, in particular a carboxylic acid group, produced the best potency.

Identification of 3-hydroxy-4[3,4-dihydro-3-oxo-2H-1,4-benzoxazin-4-yl]-2,2-dimethyldihydro-2H-benzopyran derivatives as potassium channel activators and anti-inflammatory agents

The present study described the design, synthesis and identification of 3-hydroxy-4[3,4-dihydro-3-oxo-2H-1,4-benzoxazin-4-yl]-2,2-dimethyldihydro-2H-benzopyran derivatives. Their biological activity was tested for KATP channel opener as antihypertensives, COX-1 and COX-2 activity. The results were compared with the activity of cromakalim, ibuprofen and celecoxib. The study aimed at exploring the influence of introduction of a benzoxazine substituent at position 6 of various derivatives of benzopyrans in order to improve biological activity. Several compounds were found to be equipotent or even more potent than cromakalim. Out of these nitro-substituted benzopyrans, nitro substitution at benzoxazino group possessed potent antihypertensive activity in the R/S isomers. With amino derivatives, activity remains constant when compared with standard cromakalim. Similarly, compounds 17b, 17c, 17e and 17h have exhibited around 40 % inhibition of COX-1 as compared to the inhibition of COX-2. Only two compounds 17g and 17i exhibited effective inhibition more than 50 % of COX-2 compared with the inhibition of COX-1 at a concentration of 0.3 mg/ml.

Synthesis, structure-activity relationship of novel substituted 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylates as potential anti-mycobacterial and anticancer agents

Series of 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylate derivatives 7a-7zb, 8a-8d and 9a-9d were synthesized and screened for their in vitro anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv (MTB) and cytotoxicity against three human cancer cell lines including A549, SK-N-SH and HeLa. The results indicate that six compounds are more potent and 7za is most effective anti-mycobacterial derivative compared to the standard drugs Ethambutol and Ciprofloxacin. However, 12 compounds exhibited cytotoxicity against human neuroblastoma cell line; amongst them the compound 7v is most effective compared to the standard drug Doxorubicin. This is the first report assigning in vitro anti-mycobacterial, anticancer and structure-activity relationship for this new class of 4H-chromen-1,2,3,4-tetrahydropyrimidine-5- carboxylates.

A facile demethylation of ortho substituted aryl methyl ethers promoted by AlCl3

An efficient and practical demethylation of ortho substituted aryl methyl ethers using AlCl3 has been developed. This method gives a high conversion, is simple to operate and is cost-effective. A mechanism involving the complexation of AlCl3 with the OMe and the adjacent electron withdrawing group is proposed. Many functional groups can be tolerated in the demethylation process, and 29 examples gave a demethylated product in a yield of 90-98%.