First asymmetric synthesis of (R)-desmethylsibutramine
A catalytic enantioselective addition of iBuLi to aldimine 3 derived from methyl amine and 1-(4-chlorophenyl) cyclobutanecarboxaldehyde is used as the key step in the asymmetric synthesis of (R)-desmethylsibutramine, a single enantiomer version of a pharmacologically active metabolite of anti-obesity drug sibutramine (Meridia).
Krishnamurthy, Dhileepkumar,Han, Zhengxu,Wald, Stephen A.,Senanayake, Chris H.
First preparation of enantiomerically pure sibutramine and its major metabolite, and determination of their absolute configuration by single crystal X-ray analysis
Racemic sibutramine was resolved with dibenzoyl-D-tartaric acid, and the absolute stereochemistry of sibutramine was determined by single crystal X- ray crystallography of its dibenzoyl D-tartrate. The major active metabolite (desmethylsibutramine) was ob
Fang, Qun K.,Senanayake, Chris H.,Han, Zhengxu,Morency, Cynthia,Grover, Paul,Malone, Robert E.,Bulter, Hal,Wald, Stephen A.,Cameron, T. Stanley
ENANTIOSELECTIVE SYNTHESIS OF A STERICALLY HINDERED AMINE
Compounds of the formula (I) wherein R is phenyl, or phenyl substituted by Cl, Br, C1-C4alkyl or CF3; R1 is H or methyl or ethyl; R2 is H or methyl or acyl; R3 is H or methyl; R'4/sub
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(2008/06/13)
Therapeutic agents
The present invention provides a method of treating and preventing obesity and related co-morbid conditions comprising the administration of a therapeutically effective amount of one or more monoamine reuptake inhibitors which are serotonin reuptake inhibitors and/or noradrenaline reuptake inhibitors and a 5-HT1A agonist to a patient in need thereof.
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(2008/06/13)
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