发明名称 |
ORALLY ACTIVE NONADDICTING ANALGESICS |
摘要 |
Stereoisomerically pure forms of normorphine analogs which have superior or analgesic and nonaddicting qualities are described. In addition, a method of separating diastereomeric forms of N-sec-alkyl-substituted analogs utilizes the hydrocarbyl(1-8C) diesters of the normorphine derivatives. A new method for preparing the N-methylalkylmethyl derivatives of normorphine and norcodeine and their conventional analogs is also disclosed. This method employs the corresponding methyl alkyl ketones and a reducing agent. The invention relates to compounds of the formula: (1) and the pharmaceutically acceptable acid addition salts thereof. wherein Y is OH or OMe; the dotted line indicates the presence or absence of a .pi. bond; X is -OH or =0; with the proviso that the dotted line indicates a .pi. bond, X must be OH; and wherein the compound of Formula 1 is in a stereoisomerically pure form which corresponds to that of N-.alpha.-methylcyclopropylmethyl normorphine which melts at 188-189.degree.C. |
申请公布号 |
CA1313868(C) |
申请公布日期 |
1993.02.23 |
申请号 |
CA19870532714 |
申请日期 |
1987.03.23 |
申请人 |
SRI INTERNATIONAL |
发明人 |
LAWSON, JOHN A.;DEGRAW, JOSEPH I.;LOEW, GILDA H. |
分类号 |
C07D489/00;A61K31/485;A61P25/04;C07D489/02 |
主分类号 |
C07D489/00 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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