发明名称 |
INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF |
摘要 |
A production method of an optically active 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine which is useful as an intermediate for synthesizing a pharmaceutical agent is provided and the method comprises the following steps 1) to 4): 1) reacting a bromophenylmorpholine with a hexacyanoferrate(II) or a hydrate thereof at a temperature of from 110° C. to 140° C. in a reaction mixture comprising a Na2CO3, an organophosphorus compound, and a palladium catalyst in a polar aprotic solvent alone or combination of a polar aprotic solvent and other polar aprotic solvent or hydrocarbon solvent to give a cyanophenylmorpholine; 2) reacting the cyanophenylmorpholine with hydroxylamine or hydroxylamine hydrochloride at a temperature of from 10° C. to 40° C. in an aprotic polar solvent to give a hydroxylamine derivative; 3) reacting the hydroxylamine derivative with an acylation reagent selected from the group consisting of aliphatic acyl halides, aromatic acyl halides, aliphatic acyl anhydrides and aromatic anhydrides; and 4) keeping the mixture obtained after step 3) at a temperature of from 60° C. to 140° C. to give a 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine. |
申请公布号 |
US2012059165(A1) |
申请公布日期 |
2012.03.08 |
申请号 |
US201013255748 |
申请日期 |
2010.03.09 |
申请人 |
FURUYA RIKIZOU;OZAWA HIROKI;TOYOFUKU EIJI;KUSAKA SHINICHI;IWAMURA HIROSHI;SAKAI DAIKI;NAKAYAMA KAZUKI;WATANABE KAZUTOSHI;SANOFI |
发明人 |
FURUYA RIKIZOU;OZAWA HIROKI;TOYOFUKU EIJI;KUSAKA SHINICHI;IWAMURA HIROSHI;SAKAI DAIKI;NAKAYAMA KAZUKI;WATANABE KAZUTOSHI |
分类号 |
C07D413/10;C07D413/14 |
主分类号 |
C07D413/10 |
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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