摘要 |
Furoindole derivs. of formula (I) [R=H, alkyl or alkoxy, halo or nitro; R1=alkyl, Ph or Bz; R2=alkyl; R3=COOA, Tet or CONHTet; A=H, alkyl or metal or amine cation; Tet=1H-tetrazo-5-yl are prepd. Thus, Me-3-hydroxy-5-methoxy-1-phenyl-1H-indole-2-carboxylate is alkylated with BrCH3CO2Me and the product cyclized to give 74% I [R=MeO, R1=Ph, R2=H, R3=CO2Me), which is methylated and sapond to give 85% I(R=MeO, R1=Ph, R2=Me, R3=CO2H). (I) have antiallergic activity and can be formulated for oral or parenteral administration, esp. at daily dosage of 0.5-25mg/kg.
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