SYNTHESIS OF INDOLE-CONTAINING SPLA2 INHIBITORS

摘要

A method of making a compound include reacting a compound represented by formula (I), with a base, to form the compound of formula (II); and where R1 is H, R10 or -C(O)R10; R2 is R20 -OR20, -SR20, -NR20R20' 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; each R' and R20' is individually H, alkyl, alkenyl, alkynyl, aryl or heterocyclic radical; and W is a trisubstituted phosphorous. The method provides an alternative route to indole-3-glyoxylamide compounds.