A PRACTICAL ONE POT SYNTHESIS OF 2-[2-(PYRIDYLMETHYL)-THIO]-1H-BENZIMIDAZOLES

ABSTRACT

A combination of Et₃N and pTSCl was found to be far superior than pTSCl or benzene sulfonyl chloride alone in converting substituted 2-picoline-N-oxides to the corresponding 2-chloromethylpyridines and has been exploited for the synthesis of a variety of 2-[2-(pyridylmethyl)-thio]-1H-benzimidazoles, key intermediates in the manufacture of H⁺/K⁺-ATPase inhibitors in a single pot.

Keywords:

• Omeprazole
• Lansoprazole
• Benzimidazole
• 2-Halomethylpyridines
• Pyridylmethylthiobenzimidazoles

ACKNOWLEDGMENT

The authors wish to thank Dr. N. L. Gupta and Dr. B. N. Roy for constant encouragement and Mr. Ajay K. Tiwari and Mr. Charles D'souza for their expert assistance in the preparation of the manuscript.