[EN] SYNTHESIS OF INDOLE-CONTAINING SPLA2 INHIBITORS<br/>[FR] SYNTHESE D'INHIBITEURS SPLA2 A TENEUR EN INDOLE
申请人:LILLY CO ELI
公开号:WO2001044184A1
公开(公告)日:2001-06-21
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.
一种制备化合物的方法包括将式(I)所表示的化合物与碱反应,形成式(II)的化合物;其中R1为H,R10或-C(O)R10;R2为R20-OR20,-SR20,-NR20R20'或-C(O)R20;R3,R4,R5,R6和R7各自为H,卤素,R,-OR,-SR,-NRR',-C(O)R,-C(O)OR,-S(O)R或-S(O)2R;前提是R4和R5中至少有一个不是H;每个R,R10和R20分别是烷基,烯基,炔基,芳基或杂环基;每个R'和R20'分别为H,烷基,烯基,炔基,芳基或杂环基;W为三取代
磷。该方法提供了一种合成
吲哚-3-甘氧酰胺化合物的替代路线。