ピペラジン誘導体の研究(第3報) : Piperazinoalkyltheophylline誘導体の合成

概要

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In order to examine their pharmacological activity on the circulatory system, some piperazinoalkyltheophylline derivatives (X, XI, XIV, XV) were synthesized. X, XI, and XIV were obtained by the reaction of 7-(ω-halogenoalkyl) theophyllines (VIII, IX) and 7-(2,3-epoxypropyl) theophylline (XII) with monosubstituted piperazines (I), and also by the reaction of theophylline with unsymmetrically 1,4-disubstituted piperazines (II, III, IV, V) with a functional group in ω-position. Application of 0.5 equivalent of VIII and XII to piperazine afforded 7-piperazinoalkyl-(and 2-hydroxypropyl)-theophyllines (XVI and XVII) which were reacted with halogenide (XXI) to form X and XIV. XVI and XVII were obtained by the hydrolysis of X and XIV having a carbonyl-containing substituent in the 4-position of piperazine, and subsequent application of hydrogen bromide. Reaction of piperazine with 2 equivalents each of VIII and XII afforded the corresponding bis compounds (XVIII and XIX).
公益社団法人日本薬学会の論文
1969-05-25