14545-23-4Relevant articles and documents
Bernasconi et al.
, p. 1184 (1963)
The synthesis of labelled forms of saquinavir
Wiltshire,Prior,Dhesi,Trach,Schlageter,Schoenenberger
, p. 1103 - 1126 (2007/10/03)
The development of the HIV-protease inhibitor, saquinavir (Ro 31-8959), required a range of analytical methods for the measurement of the parent drug and drug-related material in biological fluids. This paper describes the synthesis of 14-carbon and tritium labelled compounds used for in vivo and in vitro investigations of the absorption and disposition of saquinavir in animals and man. It also discusses the preparation of saquinavir labelled with deuterium and stable isotopes of carbon and nitrogen. These forms of the drug were needed for bioequivalence studies in which HPLC/MS/MS was employed for the measurement of plasma concentrations. Finally, the synthesis of a 125-iodine labelled tracer used in a radioimmunoassay for saquinavir is described.
Preparative supercritical deuterium exchange in arenes and heteroarenes
Junk, Thomas,Catallo, W. James
, p. 3445 - 3448 (2007/10/03)
Deuterated homo- and heterocyclic aromatic substrates bearing various functionalities were prepared by isotope exchange in supercritical deuterium oxide, with little or no formation of byproducts. Equilibration was attained rapidly (1-24 hrs), and deuterium exchange extended to alpha positions of alkyl homologs. Nitro- and haloarenes, thioethers, telluroethers, and some heterocyclic substrates were unstable.
