- Novel method for preparing iludoline intermediate
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The invention discloses a preparation method of a pharmaceutical intermediate, 4-(aminocarbonyl)-N-[(1,1-dimethylethoxy)carbonyl]-2,6-dimethyl-L-phenylalanine methyl ester, for treating irritable bowel syndrome (IBS-D). The preparation method comprises the following steps: with 4-iodine-3,5-dimethyl benzoic acid as a raw material, protecting carboxyl through a group, carrying out Negishi couplingreaction under the catalysis of Pd2(dba)3, removing the carboxyl protecting group, and forming active ester to react with ammonia water, thereby obtaining the product. The invention provides a novel synthetic route for a drug intermediate for treating irritable bowel syndrome (IBS-D); the reaction conditions are easy to control, the post-treatment operation is simple, and industrial production canbe smoothly realized.
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- PROCESS FOR THE PREPARATION OF OPIOID MODULATORS
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The present invention is directed to novel processes for the preparation of opioid modulators (agonists and antagonists) and intermediates in their synthesis. The opioid modulators are useful for the treatment and prevention of as pain and gastrointestina
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Page/Page column 32
(2008/06/13)
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- A convenient, large-scale synthesis of 4′-carboxamido N-Boc-2′,6′-dimethyl-l-phenylalanines
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A large-scale synthesis of a series of 4′-carboxamido N-Boc-2′,6′-dimethyl-l-phenylalanines is described. This method features mild reaction conditions and high chemical yields from commercially available N-Boc-2′,6′-dimethyl-l-tyrosine methyl ester.
- Cai, Chaozhong,Breslin, Henry J.,He, Wei
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p. 6836 - 6838
(2007/10/03)
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- NOVEL COMPOUNDS AS OPIOID RECEPTOR MODULATORS
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The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may
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Page/Page column 38
(2010/02/13)
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- Novel compounds as opioid receptor modulators
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This invention is directed towards novel compounds as opioid receptor modulators, antagonists, and agonists useful for the treatment of opioid modulated disorders such as pain and gastrointestinal disorders.
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Page/Page column 32
(2010/02/05)
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