| 摘要 |
PROBLEM TO BE SOLVED: To obtain an unknown pyridone derivative which has retrovirus protease-inhibitory action and is useful in treatment for AIDS and the like. SOLUTION: This pyridone derivative is represented by formula I (A is -SO-, -SO2 -; R<1> is an alkyl, an aryl; R<2> is H, cycloalkyl; R<3> is H, hydroxyl group; R<4> and R<5> are each H, an alkyl), typically 3-(α-cyclopropyl-3-aminobenzyl)-4- hydroxy-5,6,7,8,9,10hexahydrocyclooacta[b]pyridine-2-one. The compound of formula I is prepared by converting the pyran ring in the compound of formula II into the pyridine ring with ammonia in an organic solvent such as methanol at room temperature or with heating to give a compound of formula III and by treating the product of formula III with sulfonyl chloride or an acid chloride in an organic solvent such as methylene chloride in the presence of a base such as pyridine under ice cooling to refluxing into an acid amide.
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