| 摘要 |
NEW MATERIAL:A compound of formula I {R1 and R2 are each CH3 or OCH3; n is 0-21; m is 0 or 1; Z is of formula II [R3 and R4 are each H, (substituted) alkyl, etc.], formula III [R5 is residue of alpha-amino acid or (substituted) glucosamine residue], formula IV (R6 is 1-3C divalent hydrocarbon residue) or formula V}. EXAMPLE:3-(2,3-dimethoxy-5-methyl-1,4-benzoquinone-6-yl)propionylglycine. USE:Medicines, protocollagen. Having proline hydroxylase-inhibitory effect and collagen biosynthesis-inhibitory effect, thus useful for the preventive/therapeutic agents for the organ fibrosis in mammals, antiallergic agents, etc. PREPARATION:The carboxyl group of a compound of formula VI is converted to a reactive derivative, which is then reacted with a (substituted) alpha-amino acid of formula R5-H or (substituted) glucosamine in a solvent in the presence, if needed, of an organic base, thus obtaining the compound of the formula I (where, m is 0, Z is of formula III). |
