| 摘要 |
Indoledione derivatives having high antifungal activity are provided to maintain blood concentration of virus-infected part by delaying metabolism secretion at the treatment of whole body virus infection, and facilitate delivery of drugs to the virus-infected part, so that they improve in vivo metabolism, excretion and pharmaceutical function. The indoledione derivatives represented by the formula(1) or its pharmaceutically acceptable salts have high antifungal activity, wherein R1 is C1-5 alkyl; X is C1-5 alkyl or phenyl optionally substituted by halogen, C1-5 alkyl or C1-5 alkoxy; and R2 and R3 are each independently C1-5 alkyl, and form aromatic 6-membered hetero ring containing a nitrogen atom together. A method for preparing the indoledione derivatives represented by the formula(1a) or its pharmaceutically acceptable salts comprises the steps of: (a) reacting compounds represented by the formula(19) with C1-5 alkyl cyanoacetate in alcohol at room temperature to 100 deg. C for 2-6 hours to prepare compounds represented by the formula(20); and (b) reacting the compounds represented by the formula(20) with C1-5 alkylamine or phenylamine optionally substituted by halogen, C1-5 alkyl or C1-5 alkoxy in alcohol at room temperature for 2-5 hours, wherein R'2 and R'3 are each independently C1-5 alkyl.
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