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公开(公告)号:US20110160463A1
公开(公告)日:2011-06-30
申请号:US12999961
申请日:2009-06-16
申请人: George A. Moniz , Matthew J. Frizzle , Charles Bernard , Michael Martinelli , Margaret Faul , Jay Larrow , Karl B. Hansen , Liane Klingensmith
发明人: George A. Moniz , Matthew J. Frizzle , Charles Bernard , Michael Martinelli , Margaret Faul , Jay Larrow , Karl B. Hansen , Liane Klingensmith
IPC分类号: C07D277/14
CPC分类号: C07D277/54 , C07D263/48 , C07D277/42
摘要: The present invention relates to methods of making compounds that inhibit 11-β-hydroxysteroid dehydrogenase type 1 enzyme (11-β HSD1). One method comprises (a) contacting a compound of formula (II) with a chiral base, deprotonating agent, and an alkylating agent R3-LG, (b) contacting the product of (a) with an acid to form a salt, and (c) reacting the salt with a base to form the compound of formula (I); wherein Z, R1, R2, and R3 are defined herein.
摘要翻译: 本发明涉及制备抑制11-&bgr-羟基类固醇脱氢酶1型酶(11-和bgr; HSD1)的化合物的方法。 一种方法包括(a)使式(II)化合物与手性碱,去质子化剂和烷基化剂R3-LG接触,(b)使(a)的产物与酸形成盐,和 c)使所述盐与碱反应以形成式(I)化合物; 其中Z,R 1,R 2和R 3在本文中定义。
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公开(公告)号:US08536345B2
公开(公告)日:2013-09-17
申请号:US12999961
申请日:2009-06-16
申请人: George A. Moniz , Matthew J. Frizzle , Charles Bernard , Michael Martinelli , Margaret Faul , Jay Larrow , Karl B. Hansen , Liane Klingensmith
发明人: George A. Moniz , Matthew J. Frizzle , Charles Bernard , Michael Martinelli , Margaret Faul , Jay Larrow , Karl B. Hansen , Liane Klingensmith
IPC分类号: C07D277/54
CPC分类号: C07D277/54 , C07D263/48 , C07D277/42
摘要: The present invention relates to methods of making compounds that inhibit 11-β-hydroxysteroid dehydrogenase type 1 enzyme (11-β HSD1). One method comprises (a) contacting a compound of formula (II) with a chiral base, deprotonating agent, and an alkylating agent R3-LG, (b) contacting the product of (a) with an acid to form a salt, and (c) reacting the salt with a base to form the compound of formula (I); wherein Z, R1, R2, and R3 are defined herein.
摘要翻译: 本发明涉及制备抑制11-β-羟基类固醇脱氢酶1型酶(11-βHSD1)的化合物的方法。 一种方法包括(a)使式(II)化合物与手性碱,去质子化剂和烷基化剂R3-LG接触,(b)使(a)的产物与酸形成盐,和 c)使所述盐与碱反应以形成式(I)化合物; 其中Z,R 1,R 2和R 3在本文中定义。
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