Sanon, Csaba; Hosztafi, Sandor; Makleit, Sandor, Journal of Chemical Research, Miniprint, 1997, # 12, p. 2734 - 2742
作者:Sanon, Csaba、Hosztafi, Sandor、Makleit, Sandor
DOI:——
日期:——
Two-Step Iron(0)-Mediated N-Demethylation of <i>N</i>-Methyl Alkaloids
作者:Gaik B. Kok、Cory C. Pye、Robert D. Singer、Peter J. Scammells
DOI:10.1021/jo1008492
日期:2010.7.16
A mild and simple two-step Fe(0)-mediated N-demethylation of a number of tertiary N-methyl alkaloids is described. The tertiary N-methylamine is first oxidized to the corresponding N-oxide, which is isolated as the hydrochloride salt. Subsequent treatment of the N-oxide hydrochloride with iron powder readily provides the N-demethylated amine. Representative substrates include a number of opiate and tropane alkaloids. Key intermediates in the synthesis of semisynthetic 14-hydroxy pharmaceutical opiates such as oxycodone and oxymorphone are also readily N-demethylated using this method.
ORALLY ACTIVE NONADDICTING ANALGESICS
申请人:SRI INTERNATIONAL
公开号:EP0486671A1
公开(公告)日:1992-05-27
US4261883A
申请人:——
公开号:US4261883A
公开(公告)日:1981-04-14
[EN] ORALLY ACTIVE NONADDICTING ANALGESICS
申请人:——
公开号:WO1991018606A2
公开(公告)日:1991-12-12
[EN] Analgesic compositions containing stereoisomerically pure normorphine and norcodeine derivatives or pharmaceutically acceptable acid addition salts thereof are described. Methods of administering the novel compositions to achieve analgesia are described as well. [FR] Compositions analgésiques contenant des dérivés de normorphine et de norcodéine stéréoisomériquement purs ou leurs sels d'addition d'acide pharmaceutiquement acceptables. L'invention concerne également des procédés d'administration des nouvelles compositions permettant d'obtenir une analgésie.