- METHOD FOR PRODUCING 3-METHYL-2-THIOPHENECARBOXYLIC ACID
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A method for producing 3-methyl-2-thiophenecarboxylic acid is provided. A method for producing 3-methyl-2-thiophenecarboxylic acid, which comprises reacting a compound represented by the formula (I): (wherein X is a chlorine atom or a bromine atom) with magnesium in the presence of an alkyl halide to give a Grignard reagent represented by the formula (II): (wherein X is the same as defined above), reacting the Grignard reagent of the formula (II) with carbon dioxide, and acidifying the reaction product.
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Page/Page column 5-6
(2011/04/18)
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- Phosphorylamides, their preparation and use
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A phosphorylamide derivative represented by the general formula (I): STR1 wherein R represents an amino group that may be substituted, or a salt thereof, possesses potent antibacterial activity against Helicobacter bacterium, especially Helicobacter pylori, and is useful for prevention or treatment of digestive diseases caused by Helicobacter bacterium, solely or in combination with an antacid or an acid secretion inhibitor.
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- NOVEL HALOGENATION OF THIOPHENES WITH BENZENESELENINYL CHLORIDE AND ALUMINUM HALIDE
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In the presence of aluminum halide, benzeneseleninyl chloride is an efficient regioselective halogenating reagent for heterocyclic compounds such as thiophene, 2-methylthiophene, 3-methylthiophene, 2,5-dimethylthiophene, and furan.In the case of pyrrole, no halogenated product was obtained.A plausible reaction mechanism involving a positive halogen intermediate is proposed.
- Kamigata, Nobumasa,Suzuki, Takashi,Yoshida, Masato
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- Derivatives of thiophene-2-carboxylic acid and their pharmaceutically acceptable acid or base addition salts and use in treatment of conditions caused by thromboxane A2
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The disclosure is directed to new derivatives of thiophene-2-carboxylic acid and the pharmaceutically acceptable acid or base addition salts thereof as well as to the process for the preparation thereof. The compounds of the invention have the structural formula STR1 in which R in position 3 or 4 of the thiophene nucleus is hydrogen, methyl, chlorine or bromine and R1 is hydrogen or C1 -C4 -alkyl. The compounds have a remarkably strong inhibitory effect on the thromboxane synthetase and are useful for the treatment of conditions such as inflammation, hypertension, thrombus, apoplexy, asthma, angina pectoris, ischemic heart diseases, ischemic conditions, migraine and vascular complications in connection with diabetes.
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