1612250-64-2Relevant academic research and scientific papers
A scalable route to the SMO receptor antagonist SEN826: Benzimidazole synthesis via enhanced in situ formation of the bisulfite-aldehyde complex
Betti, Matteo,Genesio, Eva,Marconi, Guido,Sanna Coccone, Salvatore,Wiedenau, Paul
, p. 699 - 708 (2014)
A practical and scalable route to the SMO antagonist SEN826 1 is described herein, including the discussion of an alternative approach to the synthesis of the target molecule. The optimized route consists of five chemical steps. A new and efficient access to the key intermediate 6 via the bisulfite-aldehyde complex was developed, significantly enhancing the yields and reducing costs. As a result, a synthetic procedure for preparation of multihundred gram quantities of the final product has been developed.
