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All total 13 Articles be found
All total 13 Articles be foundChemical synthesis method of 4-fluoro-2-methyl benzoic acid
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Page/Page column 4; 5, (2020/04/02)
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.
Synthesis of aryl fluorides on a solid support and in solution by utilizing a fluorinated solvent
Doebele, Marion,Vanderheiden, Sylvia,Jung, Nicole,Braese, Stefan
supporting information; experimental part, p. 5986 - 5988 (2010/10/01)
(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.
New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists
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.
scheme or table, p. 8124 - 8134 (2009/11/30)
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.
