A new [2H]-labelled α-trichloroimidate glucuronic ester for the synthesis of deuterated drug conjugates

Abstract

A new reaction pathway for the synthesis of a [(2)H]-labelled trichloroacetimidate precursor for the preparation of glucuronides is described. Therewith, stable isotope-labelled drug glucuronides become accessible on a preparative scale, which can further be used as internal standards for quantitative analysis.

Keywords: 2,3,4-[2H3]-6-Methyl-2,3,4-tri-O-isobutyryl-1-O-trichloroacetimidoyl-α-d-glucopyranuronate; 2′,3′,4′-[2H3]-Clomiphene-4-O-1′β-glucuronide; 2′,3′,4′-[2H3]-Dihydroartemisinin-12α,1′β-glucuronide; glucuronidation; stable isotope-labelled internal standard.