- Asymmetric amination of meso-epoxide with vegetable powder as a low-toxicity catalyst
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This paper describes the scope and limitation of substrates subjected to asymmetric amination with epoxides catalyzed by a soluble soybean polysaccharide (Soyafibe S-DN), which we recently discovered from the reaction of 1,2-epoxycyclohexane with cyclopropylamine. Various meso-epoxides reacted with various amines afforded the corresponding products with good enantiomeric selectivity. Since it was found that pectin was found to have a catalytic ability after screening commercially available polysaccharides, we studied 33 different vegetable powders having pectic substances, and we found that many vegetable powders showed catalytic ability. These results should guide in using vegetable components as low-toxic catalysts for the production of pharmaceuticals.
- Asano, Tatsuhiro,Kurata, Hiroyuki,Takeuchi, Yuki,Tsuzaki, Kazuya,Wada, Koichi
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- Stereoselective Method for the Production of Clopidogrel
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The present invention relates to processes for preparing a compound of the general formula (Ia) wherein X is a halogen atom, or a pharmaceutically acceptable salt thereof, wherein a compound of the formula (II) wherein X is as defined above and Y and Z independently represent a leaving group each, is reacted with an optically active amino alcohol to form a first mixture of diastereomers.
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- Analgesic N-{2-[N'-(2-furylmethyl and 2-thienyl-methyl)-N'-alkylamino]cycloaliphatic}cyanobenzamides
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Cis- and trans-N-(2-aminocycloaliphatic)benzamide compounds of the formula STR1 e.g., N-methyl-N-[2-(N-pyrrolidinyl)cyclohexyl]-3,4-dichlorobenzamide, and their pharmaceutically acceptable salts, have been found to have potent analgesic activity, and compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in warm blooded animals, as well as methods for alleviating pain in animals with these compositions. Processes for preparing the compounds are also disclosed.
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- Analgesic N-[2-(furyl-methylamino and 2-thienylmethylamino)cycloaliphatic]be
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Cis - and trans-N-(2-aminocycycloaliphatic)benzamide compounds of the formula STR1 e.g., N-methyl-N-[2-[(2-furylmethyl)methylamino]-cyclohexyl]-3,4-dichlorobenzamide, and their pharmaceutically acceptable salts, have been found to have potent analgesic activity, and compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in warm-blooded animals, as well as methods for alleviating pain in animals with these compositions. Processes for preparing the compounds are also disclosed.
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- Analgesic N-(2-aminocycloaliphatic)benzamides
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Cis- and trans-N-(2-aminocycloaliphatic)benzamide compounds of the formula STR1 E.G., N-methyl-N[2-(N-pyrrolidinyl)cyclohexyl[3,4-dichlorobenzamide, and their pharmaceutically acceptable salts, have been found to have potent analgesic activity, and compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in warm blooded animals, as well as methods for alleviating pain in animals with these compositions. Processes for preparing the compounds are also disclosed.
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