Molecule of the Month
March 2018
Radical Deuteration with D2O

Recently, there has been a growing interest in the pharmaceutical industries to incorporate deuterium in drugs candidates to improve their metabolism and pharmacokinetic properties such as Deutetrabenazine (Austedo®). [1]
Soulard et al. have developed a selective method to deuterate iodides using D2O as cheap and easy available source of deuterium. [2] The reaction is catalyzed by a thiol and did not require any (transition) metal to give high yields and deuterium incorporations.

This work was carried out in the group of Prof. Dr. Philippe Renaud.

References:

  1. A. Mullard;
    "Deuterated drugs draw heavier backing"
    Nat. Rev. Drug. Discov., 2016, 15(4), 219-221; doi:10.1038/nrd.2016.63.
  2. V. Soulard, G. Villa, D. P. Vollmar, P. Renaud;
    "Radical Deuteration with D2O: Catalysis and Mechanistic Insights"
    J. Am. Chem. Soc., 2018, 140(1), 155-158; doi:10.1021/jacs.7b12105.