Method for obtaining derivatives of [ [(pyridil substituted)methyl]thio]benzomidazol
申请人:——
公开号:US20030036656A1
公开(公告)日:2003-02-20
The method for obtaining derivatives of [[(pyridil substituted)methyl]thio]benzomidazol (I), where each of R
1
, R
3
and R
4
, independently of each other, is hydrogen, an alkyl, alkoxy or fluorinated alkoxy of 1 to 6 carbon atoms, and R
2
is nitro, halogen, alkoxy or halogenated alkoxy of 1 to 6 carbon atoms, or a group —OR—(CH
2
)
n
—OR
8
, where n is an integer between 1 and 6 and R
8
represents hydrogen or an alkyl group with 1 to 6 carbon atoms, which involves (a) reacting an N-oxide of a methylpyridine with an anhydride of activated carboxylic acid or of sulfonic acid, and (b) reacting the intermediate formed in stage (a) with a corresponding mercaptobenzomidazol. The compounds (I) are useful in the synthesis of derivatives of [[(pyridil substituted)methyl]sulfinyl]benzomidazol, such as omeprazol, lansoprazol, rabeprazol or pantoprazol.
1
获得衍生物[[(吡啶取代)甲基]硫]苯并咪唑(I)的方法,其中R1、R3和R4各自独立,为氢、1至6个碳原子的烷基、烷氧基或氟代烷氧基,而R2为硝基、卤素、1至6个碳原子的烷氧基或卤代烷氧基,或者为—OR—(CH2)n—OR8基团,其中n为1至6之间的整数,R8代表氢或1至6个碳原子的烷基;该方法包括(a)将甲基吡啶N-氧化物与活性羧酸或磺酸的酸酐反应,以及(b)将在步骤(a)中形成的中间体与相应的巯基苯并咪唑反应。化合物(I)在合成[[(吡啶取代)甲基]亚砜基]苯并咪唑的衍生物,如奥美拉唑、兰索拉唑、雷贝拉唑或泮托拉唑方面有用。