Synthesis of [²H, ¹³C] and [¹⁴C] labeled vasopressin V_1a/V₂ receptor antagonist RWJ‐676070 and its stable labeled N‐des‐benzoyl metabolite

Copper‐Catalyzed Oxidative C−C Cleavage of Carbohydrates: An Efficient Access to Quinazolinone Scaffolds

“…No deuterium incorporation was seen in the product employing DMSO‐ d 6 as the solvent (Scheme 6c). The use of stable isotope‐labelled compounds for the study of metabolism, bioavailability and pharmacokinetic properties [15e,f] of drugs is a less explored territory and needs intensive investigation. In addition, the introduction of carbon isotopes into organic compounds helps to determine the fate of a drug in vivo , by analysing its pharmacokinetic properties and the complications involved such as its toxicity in its preclinical stage.…”

Recent developments in carbonylation chemistry using [13C]CO, [11C]CO, and [14C]CO

“…During the design of new synthetic routes toward carbon‐14 labeled pharmaceuticals, carbonylation chemistry with [ 14 C ]CO holds a key position. Installation of carbon‐14 by means other than carbonylation is available, including the classical examples of carboxylation with [ 14 C ]CO 2 or cyanation via nucleophilic [ 14 C ]cyanide . However, carboxylation often involves activation of the starting materials by halide to lithium exchange or though the generation of Grignard reagents, approaches that compromise the functional group compatibility of the synthetic intermediate.…”

Calcium carbide residue – a promising hidden source of hydrogen

“…Deuterium incorporation is in demand in organic chemistry and medicine. [77][78][79][80] The D-label provides additional information on the internal structure of molecules, 81,82 reaction mechanisms 83,84 and metabolic products. 85,86 If deuterium oxide is used for carbide hydrolysis, deuterated acetylene is released, which can be involved in many reactions transferring the two D-atoms incorporated into the acetylenic fragment (DCuCD).…”