- 2-nitro-4-trifluoromethyl-benzoic acid and preparation method of isomer thereof
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The invention discloses a 2-nitro-4-trifluoromethyl-benzoic acid and a preparation method of an isomer thereof, belongs to the technical field of organic synthesis, and solves the problems that in theprior art, raw materials for preparing a 2-nitro-4-trifluoromethyl-benzoic acid and the isomer thereof are expensive and the yield is slightly low. In order to solve the problems, the invention provides the 2-nitro-4-trifluoromethyl-benzoic acid and the preparation method of the isomer thereof. The preparation method comprises the following steps: with 4-(trifluoromethyl)benzonitrile as a raw material, performing a one-step reaction under the effect of a nitrating agent to obtain the 2-nitro-4-trifluoromethyl-benzoic acid and a 3-nitro-4-trifluoromethyl-benzoic acid. The preparation method has the advantages that the 2-nitro-4-trifluoromethyl-benzoic acid and the isomer thereof can be obtained only through the one-step reaction, the operation is simple and convenient, the reaction steps are short, the yield is high, and the 2-nitro-4-trifluoromethyl-benzoic acid and the isomer thereof are suitable for industrialized production.
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Paragraph 0037; 0039; 0041; 0043; 0045; 0047; 0049-0055
(2018/10/19)
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- Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinoline-8(4H)-one 1,1-dioxide K ATP channel openers: Discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno[3,2-b] quinolin-8(4H)-one 1,1-dioxide (A-278637), a potent KATP opener that selectively inhibits spontaneous bladder contractions
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Structure-activity relationships were investigated on a novel series of sulfonyldihydropyridine-containing KATP openers. Ring sizes, absolute stereochemistry, and aromatic substitution were evaluated for K ATP activity in guinea pig bladder cells using a fluorescence-based membrane potential assay and in a pig bladder strip assay. The inhibition of spontaneous bladder contractions in vitro was also examined for a select group of compounds. All compounds studied showed greater potency to inhibit spontaneous bladder contractions relative to their potencies to inhibit contractions elicited by electrical stimulation. In an anesthetized pig model of myogenic bladder overactivity, compound 14 and (-)-cromakalim 1 were found to inhibit spontaneous bladder contractions in vivo at plasma concentrations lower than those that affected hemodynamic parameters. Compound 14 showed approximately 5-fold greater selectivity than 1 in vivo and supports the concept that bladder-selective KATP channel openers may have utility in the treatment of overactive bladder.
- Carroll, William A.,Altenbach, Robert J.,Bai, Hao,Brioni, Jorge D.,Brune, Michael E.,Buckner, Steven A.,Cassidy, Christopher,Chen, Yiyuan,Coghlan, Michael J.,Daza, Anthony V.,Drizin, Irene,Fey, Thomas A.,Fitzgerald, Michael,Gopalakrishnan, Murali,Gregg, Robert J.,Henry, Rodger F.,Holladay, Mark W.,King, Linda L.,Kort, Michael E.,Kym, Philip R.,Milicic, Ivan,Tang, Rui,Turner, Sean C.,Whiteaker, Kristi L.,Yi, Lin,Zhang, Henry,Sullivan, James P.
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p. 3163 - 3179
(2007/10/03)
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- SUBSTITUTED PYRAZOLES, COMPOSITIONS AND USE
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Substituted pyrazole compounds are angiotensin II antagonists and therefore useful in the treatment of hypertension, and related cardiovascular disorders and ocular hypertension. These compounds have the general formula I: STR1
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- Demethyl(trifluoromethyl)actinomycins
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The synthesis of new 4-(trifluoromethyl)benzoic acid derivatives 2-10 and their coupling with amino acids and peptides 12, 13, 15 is described.They serve as precursors for the synthesis of the hitherto unknown demethyl(trifluoromethyl)actinocin dimethyl esters 11, demethyl-trifluoromethyl-actinocinyl peptides 14, 16, 18 and the demethyl-trifluoromethyl-actinomycins 17.Although spacially comparable with the methyl residues, the 4- and 6-trifluoromethyl groups have unexpected strong influences on the antibiotic and cytostatic properties of the actinomycins.The CH3/CF3 exchange makes it possible to bring NMR-analytically useful hetero nuclei into the centre of the actinomycin/DNA complex (Figure 1).
- Giencke, Astrid,Lackner, Helmut
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p. 569 - 579
(2007/10/02)
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