- Green synthesis method of 2-hydroxy-3-nitroacetophenone
-
The invention discloses a green synthesis method of 2-hydroxy-3-nitroacetophenone. The method comprises the following synthesis reaction steps: using carboxylic acid as a solvent, adding a metal saltcatalyst to m-nitroacetophenone, and performing a cataly
- -
-
Paragraph 0045-0056
(2019/01/07)
-
- Synthesis method of 2-hydroxyl-3-nitroacetophenone
-
The invention provides a synthesis method of 2-hydroxyl-3-nitroacetophenone. Starting from p-tert-butylphenol, the synthesis method is used for synthesizing the 2-hydroxyl-3-nitroacetophenone through four-step reaction including the steps of esterification, Fries rearrangement, nitrification and disproportionation in sequence. Compared with the prior art, the synthesis method has the advantages that raw materials are easy to obtain and the cost is low; a product obtained by disproportionation reaction mainly comprises the p-tert-butylphenol and can be recycled, so that a few of wastes are generated and the synthesis method is clean and environment-friendly; after the reaction is finished, the product can be recycled after being simply filtered, so that the cost is reduced and the emission of the wastes is reduced; and the target product can be obtained in a high yield, and the total yield reaches 70% to 80%.
- -
-
Paragraph 0018; 0022; 0026; 0027; 0028
(2017/04/27)
-
- 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
- -
-
Paragraph 0033; 0034; 0035
(2017/02/24)
-
- 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.
- Nirogi, Ramakrishna V. S.,Badange, Rajeshkumar,Reballi, Veena,Khagga, Mukkanti
-
p. 2117 - 2124
(2015/11/28)
-
- ANTI-HIV COMPOUNDS
-
Thiazole derivatives represented by Formula (I) are disclosed, where R1, R2, R3, A, X, Y, Z, R6 and R7 are disclosed herein. These thiazole derivatives and pharmaceutical compositions comprising these derivatives are useful in the treatment of HIV mediated diseases and conditions.
- -
-
Page/Page column 55
(2009/08/14)
-
- N-sulfamoyl-N'-benzopyranpiperidine compounds and uses thereof
-
N-sulfamoyl-N′-benzopyranpiperidine compounds of formula I and their physiologically acceptable acid addition salts, pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment and/or inhibition of glaucoma, epilepsy, bipolar disorders, migraine, neuropathic pain, obesity, type II diabetes, metabolic syndrome, alcohol dependence, and/or cancer, and related concomitant and/or secondary diseases or conditions.
- -
-
Page/Page column 7
(2008/06/13)
-
- N-SULFAMOYL-N’-BENZOPYRANPIPERIDINES AS INHBITORS OF CARBONIC ANHYDRASES
-
The present invention relates to novel N-sulfamoyl-N'-benzopyranpiperidines of general formula (I) and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the prophylaxis and/or treatment and/or prevention and/or inhibition of glaucoma, epilepsy, bipolar disorders, migraine, neuropathic pain, obesity, type II diabetes, metabolic syndrome, alcohol dependence, and/or cancer, and its concomitant and/or secondary diseases or conditions.
- -
-
Page/Page column 14
(2008/06/13)
-
- Selective fries rearrangement catalyzed by zinc powder
-
Zinc powder in the presence of N,N-dimethylformamide efficiently catalyzes the selective Fries rearrangement of acetylated phenols under microwave heating or with conventional heating using an oil bath. In some cases different products were obtained using microwave heating and conventional heating. Selective migration of the acyl group has been noted with good yields.
- Paul, Satya,Gupta, Monika
-
p. 1789 - 1792
(2007/10/03)
-
- Tricyclic compounds and drug compositions containing the same
-
Compounds having a β-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2 NR4 R4', or nitro; R6 represents hydrogen or lower alkyl; and X represents nitrogen, R9 represents hydrogen, one of R7 and R8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.
- -
-
-
- Synthesis and Biochemical Evaluation of a Series of Aminoflavones as Potential Inhibitors of Protein-Tyrosine Kinases p56lek, EGFr, and p60v-src
-
A series of nitroflavones, 8a-p, and their corresponding aminoflavone hydrochloride salts, 10a-p, was synthesized.The preparation of nitroflavones 8b-i,o,p began with commercially available o-hydroxyacetophenones 2b-f which were converted to o-hydroxynitroacetophenones 3a-h via a variety of nitration methods, followed by condensation with nitrobenzyl chlorides and cyclization under acidic condition.The nitroflavones 8a,j-n were prepared by nitration of the corresponding flavones 7a-e.These new compounds were evaluated for their abilities to inhibit the in vitro protein-tyrosine kinase activities of p56lek, EGFr, and p60v-src, and all of the active compounds were amino-substituted flavones.None of the nitroflavones inhibited the enzymes.The most active substance in this series against p56lek was compound 10j, which had an IC50 of 18 μM.When tested versus EGFr, compounds 10a,m displayed IC50's of 8.7 and 7.8 μM, respectively.Against p60v-src, 10a,m showed IC50 values of 28.8 and 38.4 μM, respectively.
- Cushman, Mark,Zhu, Helen,Geahlen, Robert L.,Kraker, Alan J.
-
p. 3353 - 3362
(2007/10/02)
-
- QUINOLINYL-BENZOPYRAN DERIVATIVES AS ANTAGONISTS OF LEUKOTRIENE D4
-
This invention relates to certain quinolinyl-benzopyran compounds and their use as valuable pharmaceutical agents, particularly as lipoxygenase inhibitors and/or leukotriene antagonists and/or mediator release inhibitors possessing anti-inflammatory and anti-allergic properties.
- -
-
-
- QUINOLINYL-CHROMONE DERIVATIVES AND USE FOR TREATMENT OF HYPERSENSITIVE AILMENTS
-
This invention relates to certain quinolinyl-chromone compounds and their use as valuable pharmaceutical agents, particularly as lipoxygenase inhibitors and/or leukotriene antagonists possessing anti-inflammatory and anti-allergic properties.
- -
-
-
