|Dr. Mahesh Paudyal, co-author of the science paper|
Jat et al. have developed a direct and simple one-step method for preparing N–H and N–Me aziridines from alkenes under mild conditions that avoids the need for an N-protecting group (Science,2014, 343, 61). This aziridination method involves the reaction of an alkene with the aminating agents DPH (dinitrophenyl-hydroxylamine) or N–Me–DPH in the presence of a rhodium catalyst, which produces N–H or N–Me aziridines at ambient temperature.
The simple route to aziridines can will help medicinal and natural products chemists © Science/AAAS
“The major challenge now is to develop an asymmetric version of this reaction that will selectively provide a single mirror-image form (enantiomer). This is extremely important in synthesizing drug molecules because two enantiomers of a molecule show different biological activities,” says Mahesh Paudyal, a co-author of the paper at the University of Texas Southwestern Medical Center.
[For detailed understanding and coverage: Please see “This week in Science (page 5) and Perspective (page 34)” of the same issue of Science, Chemistry World – January 9, 2014 (online), C&EN News- January 6, 2014 (online)]