鎮痙剤の研究(第3報)2位置換Quinolizidine類の簡便な新合成法とそれらの立体構造について
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概要
- 論文の詳細を見る
A new convenient synthesis of 2-substituted quinolizidines was developed. Basecatalyzed cyclization of 4-(2-chloromethylpiperidin-1-yl) butyronitrile (14) afforded 2-cyanoquinolizidines (17a and 17b), which were converted to 2-ethoxycarbonyl- (18a and 18b), 2-benzoyl- (19a and 19b) and 2-thenoylquinolizidines (20a and 20b). Quinolizidine (18a) was transformed via diarylmethanol derivatives (21a and 22a) into 5-alkyl-2-diarylmethylenequinolizidinium bromides (2), which exhibit potent anticholinergic activities. 2-Ethoxycarbonyl- (18a and 18b) and 2-benzoyl-quinolizidines (19a and 19b) were also obtained by cyclization of the chloroester (15) and the chlorobenzoyl derivative (16), respectively. The stereochemistry of all 2-substituted quinolizidines synthesized here was established.
- 社団法人日本薬学会の論文
- 1980-01-25
著者
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加藤 日出男
北陸製薬株式会社
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小川 信男
北陸製薬株式会社中央研究所研究開発本部
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越中 栄一
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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越中 栄一
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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花岡 美代次
金沢大学薬学部
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