AZIDE CYCLIZATION-BASED SYNTHESIS AND INTERMEDIATES FOR SPLA2 INHIBITORS

摘要

A process of preparing sPLA2 inhibitor compounds of formula (X)via an azide cyclization reaction that forms the intermediate indole compounds of formula (II) wherein R2 is R20, -OR20, -SR20, -NR20R20', -C(O)OR20, or -C(O)R20; R3, R4, R5, R6 and R7 are each individually H, halogen, R, -OR, -SR, -NRR', -C(O)R, -C(O)OR, -S(O)R or -S(O)2R; provided that at least one of R4 and R5 is not H; each R, R10 and R20 is individually alkyl, alkenyl, alkynyl, aryl or heterocyclic radical; and each R' and R20' is individually H, alkyl, alkenyl, alkynyl, aryl or heterocyclic radical. The method provides an alternative route to indole-3-glyoxyamide compounds.