- Phenylenediamine urotensin-II receptor antagonists and CCR-9 antagonists
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The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.
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- Reactions of benzyl aryl sulfides with excess active halogen reagents
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1,2,3-Tribromopyrrolo[1,2-b][1,2]benzothiazin-10-one (2) is produced from 2-[2-(benzylthio)benzoyl]-pyrrole (1) when treated with excess (5 equiv) NBS in CHCl3. With NCS, a mixture is obtained in which di- and trichloropyrrolo[1,2-b][1,2]benzothiazin-10-ones are present. If ethanol is present in the NCS reaction, compound 4 is formed as the major product. Further, compound 3 is also formed by the reaction of compound 1 or the corresponding disulfide with excess SOCl2. A novel route to alkyl arenesulfinic esters is also reported. Treatment of a benzyl aryl sulfide with excess (5 equiv) NCS in the presence of an n-alkyl alcohol (7 equiv) produces an n-alkyl arenesulfinic ester in good yield. An arenesulfonyl chloride is the major product in the presence of benzyl alcohol.
- Xia, Mingde,Chen, Shaowu,Bates, Dallas K.
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p. 9289 - 9292
(2007/10/03)
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- Process for the preparation of 2-fluorobenzonitrile from saccharin
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The present invention relates to a process for the preparation of 2-fluorobenzonitrile. The process comprises the steps of: (a) heating saccharin and phosphorus pentachloride under conditions and for a time sufficient to provide 2-cyanobenzenesulfonyl chloride; and (b) reacting the 2-cyanobenzenesulfonyl chloride with alkali metal fluoride in solvent for said 2-cyanobenzenesulfonyl chloride under conditions and for a time sufficient to provide 2-fluorobenzonitrile. The present invention provides a process for the preparation of 2-fluorobenzonitrile which is a versatile intermediate for a variety of 2-fluoro substituted benzenes. For example, hydrolysis of 2-fluorobenzonitrile leads to 2-fluorobenzoic acid or 2-fluorobenzamide while reduction of 2-fluorobenzonitrile leads to 2-fluorobenzylamine. Also, the reaction of 2-fluorobenzonitrile with organometallic reagents results in various 2-fluorophenyl ketones.
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