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Waser M.,DSM Fine Chemicals Austria Nfg GmbH | Obermuller R.,DSM Fine Chemicals Austria Nfg GmbH | Wiegand J.M.,DSM Fine Chemicals Austria Nfg GmbH | Schiek W.,DSM Fine Chemicals Austria Nfg GmbH | And 2 more authors.
Organic Process Research and Development | Year: 2010

2-(Pyridin-2-ylmethanesulfinyl)-1H-benzimidazole-based drugs belong to the most prominent and successfully applied proton pump inhibitors. To fulfill the demand for a flexible and safe procedure for the synthesis of early-stage intermediates which are known to possess a strong exothermal decomposition potential, we have developed a high-yielding telescoped procedure for the synthesis of a key intermediate in the synthesis of these drugs. This strategy turned out to be highly reproducible in laboratory as well as on pilot-plant scale. As the starting material, as well as some of the intermediates, shows a highly exothermal decomposition potential, extensive safety investigations were undertaken. The whole process was adapted in a safe and reliable manner based on the outcome of this systematic approach. Considering these precautions, no safety issues were observed, neither in the laboratory nor in the pilot plant. © 2010 American Chemical Society. Source

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