New procedure to mask the 2,3-pi bond of the indole nucleus and its application to the preparation of potent opioid receptor agonists with a Corynanthe skeleton |
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Authors: | Takayama Hiromitsu Misawa Kaori Okada Naoki Ishikawa Hayato Kitajima Mariko Hatori Yoshio Murayama Toshihiko Wongseripipatana Sumphan Tashima Kimihito Matsumoto Kenjiro Horie Syunji |
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Affiliation: | Graduate School of Pharmaceutical Sciences, Chiba University, Chiba 263-8522, Japan. takayama@p.chiba-u.ac.jp |
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Abstract: | Treatment of indole alkaloids with hypervalent iodine in the presence of ethylene glycol provides 2,3-ethylene glycol bridged adducts that could be converted into the original indoles under mild reductive conditions. This procedure, which involves masking of the reactivity of the indole nucleus at the beta-position, was utilized for the modification of the benzene ring of the indoline derivative and was applied to the preparation of potent opioid receptor agonists with the Corynanthe skeleton. [reaction: see text] |
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