| 摘要 |
PURPOSE:To provide the subject compound having an N-methyltyrosine and alanine-containing cyclic hexapeptide structure, extracted from Rubia akane, exhibiting an immunosuppressive action, and useful for treating autoimmune diseases such as chronic articular rheumatism and systemic lupus erythematosus. CONSTITUTION:A compound having an N-methyltyrosine and alanine-containing cyclic hexapeptide structure of the formula (R<1> is OCH3; R<2> is OH, OCH3) and extracted from Rubia akane a kind of medicinal plant, is treated with boron tribromide in an argon atmosphere at -78 deg.C in dichloromethane, and the derived compound in which R1, R2 are hydroxy groups is treated with N- phenyltrifluoromethane sulfonamide and triethylamine in an argon atmosphere at room temperature, and if necessary, further treated with triethylamine, palladium acetate, 1,1'-bis(diphenylphosphine)-ferrocene, formic acid, etc., to obtain the objective compound of the formula (one of R<1>, R<2> is H, and the other is H, OH, lower alkoxy). |
