发明名称 Production of 3-hydroxymethyl-quinuclidine useful as intermediate for antihistamine mequitazine
摘要 Production of 3-hydroxymethyl-quinuclidine (I) comprises either (A) converting 3,3-methyleneoxy-quinuclidine (II) or 3-quinuclidinone (IV) to 3-methoxymethyl-3-quinuclidinol (IV), converting (IV) to 3-formyl-quinuclidine (V), and reducing (V) to (I), or (B) converting (IV) to 3-cyano-quinuclidine (VI), hydrolyzing (VI) to quinuclidine-3-carboxylic acid (VII) and reducing (VII) to (I). Production of 3-hydroxymethyl-quinuclidine of formula (I) comprises either: (A) converting 3,3-methyleneoxy-quinuclidine of formula (II) or 3-quinuclidinone of formula (IV) to 3-methoxymethyl-3-quinuclidinol of formula (IV), converting (IV) to 3-formyl-quinuclidine of formula (V), and reducing (V) to (I); or (B) converting (III) to 3-cyano-quinuclidine of formula (VI), hydrolyzing (VI) to quinuclidine-3-carboxylic acid of formula (VII) and reducing (VII) to (I): An Independent claim is also included for 3-methoxymethyl-3-quinuclidinol of formula (IV).
申请公布号 FR2777278(A1) 申请公布日期 1999.10.15
申请号 FR19980004451 申请日期 1998.04.09
申请人 PIERRE FABRE MEDICAMENT 发明人 GUMINSKI YVES;IMBERT THIERRY;LESIMPLE PATRICK
分类号 A61K31/445;C07D453/02;(IPC1-7):C07D471/08 主分类号 A61K31/445
代理机构 代理人
主权项
地址