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    • 17. 发明申请
    • NEW SYNTHESIS OF SPLA2 INHIBITORS
    • SPLA2抑制剂的新合成
    • WO0144182A3
    • 2002-03-07
    • PCT/US0032446
    • 2000-12-11
    • LILLY CO ELIBEIGHT DOUGLAS WADESAWYER JASON SCOTT
    • BEIGHT DOUGLAS WADESAWYER JASON SCOTT
    • C07D209/08C07C233/25C07C209/08C07C233/33
    • C07D209/08Y02P20/55
    • A method of making a compound, comprises deprotecting a compound of formula (I), to form the compound of formula (II); where formula (I) isand, formula (II) isand where Rr 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 P is a protecting group. The method provides an alternative route to indole-3-glyoxyamide compounds.
    • 制备化合物的方法包括使式(I)化合物脱保护,形成式(II)化合物; 式(I)和式(II)中Rr为H,R10或-C(O)R10; R2是R20 -OR20,-SR20,-NR20R20或-C(O)R20; R 3,R 4,R 5,R 6和R 7各自独立地为H,卤素,R,-OR,-SR,-NRR', - C(O)R,-C(O)OR,-S(O) S(O)2; 条件是R 4和R 5中的至少一个不是H; 每个R,R 10和R 20分别是烷基,烯基,炔基,芳基或杂环基; 每个R'和R 20'独立地为H,烷基,烯基,炔基,芳基或杂环基; 而P是保护基。 该方法提供了吲哚-3-乙酰氧基酰胺化合物的替代途径。