鎮痙作用を有するキサンテン誘導体の合成研究(第5報) : クロルキサンテン-9-酢酸アルカミンエステルについて

概要

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1-Chloroxanthen-9-ol (IIIa) was prepared by the reduction of 1-chloroxanthen-9-one (IIa) with sodium amalgam and ethanol. IIIa was condensed with malonic acid to 1-chloroxanthene-9-malonic acid (IVa), and the acid was decarboxylated to 1-chloroxanthene-9-acetic acid (Va). Cyclization of l-(m-chlorophenoxy)benzoic acid (XI) afforded a mixture (IIa') of IIa and 3-chloroxanthen-9-one, and IIa was not isolated. Therefore, IIa was prepared from 1-amino-xanthen-9-one. (Ia). 2-, 3-, and 4-Chloroxanthene-9-acetic acids (Vb-d) were prepared and their alkamine ester hydrochlorides were obtained. The anti-acetylcholine, anti-barium chloride, and anti-histamine activities of Va〜d these ester hydrochlorides were examined and it was found that the introduction of chlorine into the xanthene ring of the alkamine ester hydrochlorides of xanthene-9-acetic acid, especially into the 2-or 3-position resulted in the weakening of these activities.
公益社団法人日本薬学会の論文
1966-08-25