发明名称 2-PHENYLMORPHOLIN-5-ONE DERIVATIVE AND MEDICINE COMPOSITION CONTAINING THE SAME
摘要 PROBLEM TO BE SOLVED: To obtain the subject new compound having a phosphodiesterase IV-inhibiting action, a bronchodilatation action and an antiinflammatory action, and useful for preventing and treating inflammatory diseases, etc. SOLUTION: A compound of formula I [R1 is a (substituted) 1-8C alkyl, a (substituted) 3-7C cycloalkyl, indanyl; R2 is a 1-4C alkyl; R3 is H, a (substituted) 3-7C cycloalkyl, etc.; R4 is H, a (substituted) 1-6C alkyl, etc.; R5 , R6 are each H, a (substituted) 1-5C alkyl, a (substituted) 3-7C cycloakyl, etc.], e.g. 2-(3,4-dimethoxyphenyl)morpholin-5-one. The compound of formula I is preferably obtained e.g. through processes comprising reacting a ketone derivative of formula II with trimethylsilylcyanate in the presence of a catalytic amount of lead iodide and subsequently converting the obtained nitrile derivative of formula III into an amino alcohol compound with a reducing agent such as lithium aluminum hydride.
申请公布号 JPH10120665(A) 申请公布日期 1998.05.12
申请号 JP19970244834 申请日期 1997.08.27
申请人 NIKKEN CHEM CO LTD 发明人 INE SHINJI;YAMANA KENSHIROU;NODA KYOJI
分类号 C07D265/32;A61K31/535;A61K31/5375;A61P11/00;A61P11/08;A61P17/00;A61P29/00;A61P37/00;A61P43/00;C07D413/06;(IPC1-7):C07D265/32 主分类号 C07D265/32
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