| 摘要 |
<p>PURPOSE:To provide two kinds of the new subject carboxylic acid derivatives useful as raw materials for producing optically active compounds which are expected in the application field as an anticancer agent. CONSTITUTION:A 2,3-dihydroindole-3-carboxylic acid derivative of formula I (R<1> is H, 1-4C alkyl; R<2> is H, COOR<1>; X is two H atoms, O, S; R<3> is H, amino group-protecting group; R<4> is H, nitro, amino; R<5> is H, OH-protecting group) and a 2,3-dihydroindole-3-carboxylic acid derivative of formula II (R<6>, R<7> are H, 1-6C alkyl, benzyl, phenyl; Y, Z are O, S, substituted amino), e.g. 6- benzyloxy-3,3-di(methylcarbonyl)-2,3-dihydroindol-2-one and 6-benzyloxy-1-t- butoxycarbonyl-(3S)-hydroxymethyl-2,3-dihydro(1H)-indole. The compound of formula I is obtained from a compound of formula III through a compound of formula IV. The compound of formula II is obtained by reacting a compound of formula V with a compound of formula VI.</p> |
