The synthesis of one H-2 labeled and two H-3 labeled leukotriene C4 synthase inhibitors.
2020
: 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 [2 H6 ]acetone in a modification of the route used by medicinal chemistry.
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