| 摘要 |
<p>PURPOSE:To obtain a new low toxic compound, having water-solubility and useful as a cancerous cell metastatic suppressor. CONSTITUTION:(3S,4S,5R,6R)-6-(Trifluoroacetamino)-4,5-dihydroxypiperdi ne-3- carboxylic acid of formula I and its salts. This compound is obtained by oxidizing a compound of formula II [R<1> is H or imino-protecting group; X<1> and X<2> are hydroxyl-protecting group, etc.; R<2> is lower alkyl, aralkyl, etc.; (x) is S- configuration; (y) is R-configuration; (z) is R,S-configuration] or a mixture of the compound of formula II with a compound of formula III with oxygen in the presence of palladium chloride and cuprous chloride, providing a compound of formula IV [(w) is S-configurationl and then releasing the ester-forming group (R<2>) and further the imino-protecting group (R<1>) and hydroxyl-protecting groups (X<1> and X<2>). The compound of formula I is capable of extremely remarkably suppressing the diffusion and metastasis of a cancerous cell and usable together with the existing carcinostatic agent.</p> |
