Manufacturing of the drug substance 1

July 24, 2024

• Title:       

  Manufacturing of the drug substance 1

• Image Source:

  Development of a practical route for the manufacture of N-[5-(3-lmidazol-1-yl-4-methanesulfonyl-phenyl)-4-methyl-thiazol-2-yl]acetamide

• Mark:

  Scheme 4

• Associated context:

  A more straightforward selective benzylic chlorination process was also identified as an alternative to the previously used bromination (see Scheme 4). The keto intermediate 3 was reacted with sulfuryl chloride in acetonitrile at ca. 0 °C for 1 h,  concentrated, and directly submitted to the subsequent thiazole ring formation as previously developed.