S. Kai
2009
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Journal
Chinese Journal of Pharmaceuticals
Abstract
Palonosetron hydrochloride was synthesized by reductive amination of (3,4-dihydronaphthalen-1-yl)methylamine hydrochloride with 3-quinuclidinone hydrochloride subsequent reduction to give N-[(3,4-dihydronaphthalen-1-yl)methyl]-1-azabicyclo[2.2.2]octan-3-amine dihydrochloride,which was subjected to resolution,catalytic hydrogenation,and cyclization with triphosgene in 12% overall yield.