Synthesis and Preliminary Pharmacological Evaluation of New 6‐cyano‐2,3‐dihydro‐5H‐oxazolo[3,2‐a]pyrimidin‐5‐ones and 2‐ethyl(methylenecyanoacetate)‐2‐iminooxazolidines

C. Chaimbault, J. Bosc, C. Jarry, S. Daulouède, P. Vincendeau
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引用次数: 3

Abstract

One-step ring-annulation of 5-substituted 2-amino-2-oxazolines with diethyl ethoxymethy-lenemalonate yielded 2-substituted 6-carboethoxy-2,3-dihydro-5H-oxazolo[3,2-a]pyrimidin-5-ones. Under the same conditions 2-substituted 6-cyano-2,3-dihydro-5H-oxazolo[3,2-a]-pyrimidin-5-ones and the corresponding 2-ethyl(methylenecyanoacetate)-2-iminooxazo-lidines were obtained from ethyl ethoxymethylenecyanoacetate. Some of these compounds were evaluated in mice for antiparasitic activity.
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新型6 -氰- 2,3 -二氢- 5H -恶唑啉[3,2 - a]嘧啶- 5 -酮和2 -乙基(亚甲基氰乙酸酯)- 2 -亚胺恶唑烷的合成及初步药理评价
5-取代2-氨基-2-恶唑啉与二乙基乙氧基烯丙酸酯一步环化得到2-取代6-碳乙氧基-2,3-二氢- 5h -恶唑[3,2-a]嘧啶-5-酮。在相同条件下,从乙氧基亚甲基乙酸乙酯中得到2-取代的6-氰基2,3-二氢- 5h -恶唑[3,2-a]-嘧啶-5-酮和相应的2-乙基(亚甲基乙酸)-2-亚胺恶唑-lidines。其中一些化合物在小鼠体内的抗寄生虫活性进行了评估。
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