9-Amino-2,3,5,6,7,8-hexahydro-1H-cyclopenta[b]quinoline Monohydrochloride Monohydrate(NIK-247)推定代謝物の合成(第1報)モノオール性代謝物

概要

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The two mono-hydroxylated metabolites of 9-amino-2,3,5,6,7,8-hexahydro-1H-cyclopenta [b] quinoline monohydrochloride monohydrate (NIK-247), which is a new drug for the treatment of dementia, were synthesized to determine their chemical structures. Reduction of two tricyclic ketones, 9-amino-1,2,3,5,6,7-hexahydro-8H-cyclopenta [b] quinolin-8-one and 9-amino-2,3,5,6,7,8-hexahydro-1H-cyclopenta [b]-quinolin-1-one, with NaBH_4 afforded the corresponding racemic alcohols. The optically active mono-hydroxylated metabolites, (+)-9-amino-2,3,5,6,7,8-hexahydro-1H-cyclopenta [b] quinolin-8-ol and (+)-9-amino-2,3,5,6,7,8-hexahydro-1H-cyclopenta [b] quinolin-1-ol, were obtained by optical resolution of each racemic alcohol using (+)-di-p-toluoyl-D-tartaric acid.
社団法人日本薬学会の論文
1995-12-25