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

• Published in: Journal of labelled compounds & radiopharmaceuticals 2014-10, Vol.57 (12), p.699-703
• Main Authors: Heinkele, Georg, Geditz, Mirjam C. K., Ganchev, Boian, Kerb, Reinhold, Hofmann, Ute, Mürdter, Thomas E.
• Format: Article
• Language: English
• Subjects: 1′β-glucuronide; 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; 4-[2H3]-6-Methyl-2; 4-tri-O-isobutyryl-1-O-trichloroacetimidoyl-α-d-glucopyranuronate; 4′-[2H3]-Clomiphene-4-O-1′β-glucuronide; 4′-[2H3]-Dihydroartemisinin-12α; Acetamides - chemical synthesis; Chemistry Techniques, Synthetic - methods; Chloroacetates - chemical synthesis; Deuterium - chemistry; glucuronidation; Glucuronides - chemical synthesis; Radiopharmaceuticals - chemical synthesis; stable isotope-labelled internal standard
• ISSN: 0362-4803; 1099-1344
• DOI: 10.1002/jlcr.3243

A new reaction pathway for the synthesis of a [2H]‐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. A new reaction pathway for the synthesis of a [2H]‐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.