The synthesis of one H ‐2 labeled and two H‐3 labeled leukotriene C4 synthase inhibitors

As part of a medicinal chemistry program aimed at developing a leukotriene C4 synthase inhibitor for the treatment of asthma, two tritium labeled and one stable isotope labeled compounds were required. The synthesis of the tritium labeled compounds used a standard bromination ‐tritiodehalogentation approach. One of the tritium labeled compounds was observed to exchange its tritium label slowly with the solvent. The stable isotope labeled compound was prepared in seven steps (3% overall yield) from [2H6]acetone in a modification of the route used by medicinal chemistry.

Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 21, 2020 Category: Biochemistry Authors: Jonas Bergare, Lee Kingston, Dominic J. Guly, James Dolan, Richard J. Lewis, Charles S. Elmore Tags: RESEARCH ARTICLE Source Type: research