- Chemical synthesis method of 4-fluoro-2-methyl benzoic acid
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The invention relates to a chemical synthesis method of 4-fluoro-2-methyl benzoic acid. According to the synthesis method, m-fluorotoluene and trichloroacetyl chloride are used as starting raw materials, and are subjected to a Friedel-Crafts acylation reaction under the catalytic action of anhydrous aluminum trichloride, hydrolysis and acidification are performed under an alkaline condition to obtain two isomers of 4-fluoro-2-methyl benzoic acid and 2-fluoro-4-methyl benzoic acid, and the isomers are separated through re-crystallizing to obtain the target product 4-fluoro-2-methylbenzoic acid.The method has the advantages of accessible raw materials, mild reaction conditions and low cost, and is suitable for industrial production.
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Page/Page column 4; 5
(2020/04/02)
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- BORON-CONTAINING DIACYLHYDRAZINES
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The present disclosure provides boron-containing diacylhydrazines having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, and R5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.
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Paragraph 0541
(2014/09/29)
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- Synthesis of aryl fluorides on a solid support and in solution by utilizing a fluorinated solvent
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(Figure Presented) F for fast: The perfluorinated solvent C 6F14 is the key to a new variant of the BalzSchiemann reaction for the synthesis of fluorinated arenes. Triazenes are converted into fluoroarenes under mild con-ditions on a support and in solution (see scheme). The method is straightforward and inexpensive, and yields previously difficult-to-prepare fluoroarenes in high purity.
- Doebele, Marion,Vanderheiden, Sylvia,Jung, Nicole,Braese, Stefan
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supporting information; experimental part
p. 5986 - 5988
(2010/10/01)
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- INHIBITORS OF STEAROYL-COA DESATURASE
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.
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- New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists
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Vasopressin (AVP) is a hormone that stimulates an increase in water permeability through activation of V2 receptors in the kidney. The analogue of AVP, desmopressin, has proven an effective drug for diseases where a reduction of urine output is desired. However, its peptidic nature limits its bioavailability. We report herein the discovery of potent, nonpeptidic, benzylurea derived agonists of the vasopressin V2 receptor. We describe substitutions on the benzyl group to give improvements in potency and subsequent modifications to the urea end group to provide improvements in solubility and increased oral efficacy in a rat model of diuresis. The lead compound 20e (VA106483) is reported for the first time and has been selected for clinical development.
- Yea, Christopher M.,Allan, Christine E.,Ashworth, Doreen M.,Barnett, James,Baxter, Andy J.,Broadbridge, Janice D.,Franklin, Richard J.,Hampton, Sally L.,Hudson, Peter,Horton, John A.,Jenkins, Paul D.,Penson, Andy M.,Pitt, Gary R. W.,Rivière, Pierre,Robson, Peter A.,Rooker, David P.,Semple, Graeme,Sheppard, Andy,Haigh, Robert M.,Roe, Michael B.
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scheme or table
p. 8124 - 8134
(2009/11/30)
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- HETEROCYCLIC CONDENSED COMPOUNDS USEFUL AS ANTIDIURETIC AGENTS
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The invention concerns compounds according to general formulae 1, wherein G1 is an amine. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.
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Page/Page column 22
(2010/10/20)
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- P38 inhibitors and methods of use thereof
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This invention relates to inhibitors of p38, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders mediated by p38.
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Page/Page column 31; sheet 33
(2008/06/13)
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- benzamide derivatives as oxytocin agonists and vasopressin antagonists
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Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or Via receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.
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- NOVEL BENSOPHENONE DERIVATIVES OR SALTS THEREOF
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A benzophenone derivative represented by the following formula: whereinR1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl;R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, ???or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
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- Bicyclic vasopressin agonists
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Compounds according to general formula (1), and pharmaceutically acceptable salts thereof, wherein V is a covalent bond or NH, X is selected from CH2, O and N-alkyl, Z is either S or —CH═CH—, R1and R2are independently sele
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Page column 11
(2010/11/30)
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- Syntheses of 4-methoxymethylbenzyl permethrinates containing fluorine and their insecticidal activity
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In order to investigate the relationship between the position of fluorine atom and insecticidal activity about 4-methoxymethylbenzyl permethrinates containing fluorine, 2 and 3-fluoro-4-methoxymethylbenzyl (±)-cis-permethrinate were synthesized. Their insecticidal activities were tested and the fluorine effect of title compounds was discussed.
- Zou, Xinzhuo,Qiu, Zongxing
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p. 173 - 179
(2007/10/03)
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- Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase IB (PTP-IB)
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The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.
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- The superbase approach to flurbiprofen: An exercise in optionally site-selective metalation
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A superior route to the analgesic flurbiprofen has been devised. Key steps are the selective deprotonation of 3-fluorotoluene with tert-butyllithium in the presence of potassium tert-butoxide (LIT-KOR) at the 4-position and the selective deprotonation of the 4-methyl-2-fluorobiphenyl with lithium diisopropylamide in the presence of potassium tert-butoxide (LIDA-KOR) at the benzylic position. Depending on the reagent and the substituent pattern, the 3- and 5-positions of 2-fluorobiphenyls can also be specifically attacked.
- Schlosser, Manfred,Geneste, Herve
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p. 1969 - 1973
(2007/10/03)
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