PURPOSE: To obtain a novel compound, which is a synthetic intermediate of a strong protein kinase C inhibiting substance, useful for treatment of diabetes, or the like.
CONSTITUTION: A compound represented by formula I (wherein R2 is N3, an NH-protecting group, an amine protecting group or a hydroxy protecting group; L1 is an eliminable group; Z is (CH2)n; and (n) is 1 to 3), such as 2,3-bis-(1H- indol-3-yl)-N-methylmaleimide is produced. The compound represented by formula I is obtained by alkylating a compound represented by formula II with an organic metal reagent (for example, lithiumacetylide), and reacting the product with a compound represented by formula III (wherein R3 is a halo, a protected hydroxy, or the like; and R4 is chloro, bromo or iodo) so as to obtain a compound represented by formula IV, and converting the compound represented by formula IV by a known method. By coupling a compound represented by formula I with bisindolylmaleimide, a macrocyclic bisindolylmaleimide, which is a protein kinase C inhibiting substance, can be obtained. The protein kinase C inhibiting substance is useful for treatment of anemia, inflammation, central nervous system diseases, cardiovascular diseases, skin diseases, cancers, or the like.
UIRIAMU FURANSHISU HIISU JIYUN
MAIKERU ROBAATO JIROOSEKU
JIYON HANPUTON MAKUDONARUDO ZA
KURISUTOFUAA JIYON RITOO
REONARUDO RARII UINAAROSUKII J
Next Patent: Mechanical timepiece movement with power reserve detector