Abstract: The method for obtaining derivatives of [[(pyridil substituted)methyl]thio]benzomidazol (I), where each of R1, R3 and R4, independently of each other, is hydrogen, an alkyl, alkoxy or fluorinated alkoxy of 1 to 6 carbon atoms, and R2 is nitro, halogen, alkoxy or halogenated alkoxy of 1 to 6 carbon atoms, or a group —OR—(CH2)n—OR8, where n is an integer between 1 and 6 and R8 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.

Abstract: The present invention relates to a procedure for the oxidation of a thioether group to a sulfoxide group, with aqueous sodium percarbonate in the presence of a molybdenum salt as a catalyst. The procedure is of application to oxidize the thioether group of a compound (I), where R1 is a C1-C6 alkyl, a halogenated C1-C6 alkyl, or —(CH2)n—OR9, where n is an integer between 1 and 6 and R9 is H or a C1-C6 alkyl; R2, R3, R4, R5, R6 and R8, independently form each other represent H, a C1-C6 alkyl, or C1-C6 alkoxy; and R7 is H, a C1-C6 alkyl, a C1-C6 alkoxy or a C1-C6 fluorinated alkoxy, in order to obtain the sulfinyl derivative (II).

Abstract: The method for obtaining derivatives of [[(pyridil substituted)methyl]thio]benzomidazol (I), where each of R1, R3 and R4, independently of each other, is hydrogen, an alkyl, alkoxy or fluorinated alkoxy of 1 to 6 carbon atoms, and R2 is nitro, halogen, alkoxy or halogenated alkoxy of 1 to 6 carbon atoms, or a group —OR—(CH2)n—OR8, where n is an integer between 1 and 6 and R8 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.

Abstract: The present invention relates to a procedure for the oxidation of a thioether group to a sulfoxide group, with aqueous sodium percarbonate in the presence of a molybdenum salt as a catalyst. The procedure is of application to oxidize the thioether group of a compound (I), where R1 is a C1-C6 alkyl, a halogenated C1-C6 alkyl, or —(CH2)n—OR9, where n is an integer between 1 and 6 and R9 is H or a C1-C6 alkyl; R2, R3, R4, R5, R6 and R8, independently form each other represent H, a C1-C6 alkyl, or C1-C6 alkoxy; and R7 is H, a C1-C6 alkyl, a C1-C6 alkoxy or a C1-C6 fluorinated alkoxy, in order to obtain the sulfinyl derivative (II).