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    • 1. 发明申请
    • PROCESS FOR 2-SUBSTITUTED BENZO[b]THIOPHENE COMPOUNDS AND INTERMEDIATES THEREOF
    • 2-取代苯并[b]噻吩化合物及其中间体的方法
    • WO1996030361A1
    • 1996-10-03
    • PCT/US1996004417
    • 1996-03-28
    • ELI LILLY AND COMPANYHAUSER, Kenneth, L.PALKOWITZ, Alan, D.SALL, Daniel, J.THRASHER, Kenneth, J.
    • ELI LILLY AND COMPANY
    • C07D333/52
    • C07D333/54C07D333/56C07D333/62C07F5/025Y02P20/55
    • The present invention provides processes for preparing compounds of formula (I), wherein R is -H, -OH, or OR , in which R is a hydroxy protecting group; and R is -H, -OH, or OR , in which R is a hydroxy protecting group, and for preparing compounds of formula (VII), wherein R is -H, -OH, or OR , in which R is a hydroxy protecting group; R is -H, -OH, or OR , in which R is a hydroxy protecting group; R is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; R is bromo, chloro, iodo, or an activating ester group; and n is 2 or 3. Also provided are processes for preparing compounds of formula (VII) in addition to intermediates of formula (IX), wherein R is -OH, or -OR , in which R is a hydroxy protecting group; and Z is bromo, iodo, triflate, or -B(OH)2.
    • 本发明提供制备式(I)化合物的方法,其中R 1是-H,-OH或OR 3,其中R 3是羟基保护基; 和R 2是-H,-OH或OR 4,其中R 4是羟基保护基,并且用于制备式(VII)的化合物,其中R 1是-H, - OH或OR 3,其中R 3是羟基保护基; R 2是-H,-OH或OR 4,其中R 4是羟基保护基; R 5是1-哌啶基,1-吡咯烷基,甲基-1-吡咯烷基,二甲基-1-吡咯烷基,4-吗啉代,二甲基氨基,二乙基氨基,二异丙基氨基或1-六亚甲基亚氨基; R 6是溴,氯,碘或活化酯基; 还提供了除式(Ⅸ)中间体外还制备式(Ⅶ)化合物的方法,其中R 1'是-OH或-OR 3,其中R 1, 3>是羟基保护基; 和Z是溴,碘,三氟甲磺酸酯或-B(OH)2。