Vitamins

Lewis Acid-Catalyzed Synthesis of 4-Aminopyrimidines: A Scalable Industrial Process

“…Aminopyrimidines are key intermediates for the synthesis of biologically active substances such as vitamin B 1 (thiamin 1 ), its natural antagonist bacimethrin 2 , pesticides (amprolium 3 ), and chemotherapeutic agents (trimethoprim 4 ) . Grewe diamine 5 is the key building block in all industrial syntheses of vitamin B 1 (Figure ) . Although various synthetic protocols are available for the synthesis of 4-aminopyrimidines, reports on industrially applicable syntheses remain scarce .…”

“…Grewe diamine 5 is the key building block in all industrial syntheses of vitamin B 1 (Figure ) . Although various synthetic protocols are available for the synthesis of 4-aminopyrimidines, reports on industrially applicable syntheses remain scarce . Commonly, major challenges in designing industrially attractive processes for fine chemicals include the development of low-cost, atom-efficient processes that are easily scalable, nonhazardous, and at the same time highly selective …”