- Novel 5-hydroxytryptamine (5-HT3) receptor antagonists. III. Pharmacological evaluations and molecular modeling studies of optically active 4,5,6,7-tetrahydro-1H-benzimidazole derivatives
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The R- and S-enantiomers of the 4,5,6,7-tetrahydro-1H-benzimidazole derivatives 3-8 were prepared by optical resolution. Each R-isomer, except for 3, was almost two orders of magnitude more potent than its S-isomer as a 5-hydroxytryptamine (5-HT3/su
- Ohta, Mitsuaki,Suzuki, Takeshi,Furuya, Toshio,Kurihara, Hiroyuki,Tokunaga, Tatsuhiro,Miyata, Keiji,Yanagisawa, Isao
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- NOVEL PROCESS FOR PRODUCING RAMOSETRON OR ITS SALT
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[PROBLEMS] To provide a novel process for producing ramosetron or its salt that is useful as a pharmaceutical, especially as a therapeutic and/or preventive agent for digestive symptoms caused by administration of an anti-malignant tumor agent, diarrheal-type irritable bowel syndrome, diarrheal symptoms of irritable bowel syndrome, etc. [MEANS FOR SOLVING PROBLEMS] Ramosetron or its salt can be produced by reacting any of compounds of the formula: (I) [wherein X is a halogen] or a salt thereof with 1-methyl-1H-indole in the presence of a Lewis acid selected from the group consisting of lower-alkylaluminum dihalides, di-lower-alkylaluminum halides, tri-lower-alkylaluminums and lower-alkylaluminum sesquihalides.
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(2008/06/13)
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