| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain a new 8H-thieno[2,3-b]pyrrolidin-8-one compound having an antitumor characteristic and useful for treating cancer and solid tumor. SOLUTION: A compound of formula I [R1 and R3 are each H, a halogen or the like; R2 is a (substituted) aryl or the like], for example, 3-(2- methoxyphenyl)-8H-thieno[2,3-b]pyrrolidin-8-one. The compound of formula I is obtained by reacting a compound of formula II with ethyl formate in the presence of an alkali metal, reacting the obtained compound with phenylsulfonyl chloride under a nucleophilic addition condition, reacting the obtained compound of formula III with methyl thioglycolate to protect the amino group of the compound, reacting the compound with a compound of the formula: R3-X (X is a releasing group), removing the protecting group from the amino functional group, reacting the obtained compound of formula IV with dimethoxytetrahydrofuran, etc., reacting the product with pyrrolidine and subsequently cyclizing the obtained compound of formula V with phosphorus oxychloride.</p> |
