| 摘要 |
<p>PURPOSE:To obtain the compound having an activity for blocking the neural excitation transmission of synapse. CONSTITUTION:A compound of formula I (R<1> is H, benzyl, 1-4C alkyl) and its salt, e.g. N-[3-[(3-aminopropyl)-malonylamide-1-yl]aminopropyl ]-4- benzyloxyphenylacetoamide. The compound is obtained by reacting a 4- substituted oxyphenylacetic acid (e.g. 4-benzyloxyphenylacetic acid) with a 3-N-protected-1,3-diaminopropane [e.g. 3-N-(t-butoxycarbonyl-1,3-diaminopropane], removing the amino-protecting group R<4> of the produced compound of formula II (R<1> is benzyl, 1-4C alkyl; R<4> is t-butoxycarbonyl), reacting the reaction product with an alkylmalonyl chloride, hydrolyzing the product with an alkali, reacting the produced compound of formula III with a 3-N-1,3-diaminopropane, and further removing the amino group-protecting group.</p> |
