Practical synthesis of thio-cotarnine analogues

Abstract

Sulfur-based tetrahydro-isoquinoline is rarely accessible in the literature, but its synthesis is attractive due to its importance in medicinal chemistry and the pharmaceutical industry. The very first example of thio-cotarnine derivatives under metal- and base-free conditions has been reported here. It provides a general method for synthesizing sulfur derivatives of cotarnine. Thio-tetrahydroisoquinoline was synthesized at gram scale by a greener protocol. All the new compounds synthesized are of biological interest and are under investigation.