Satzinger G
Arzneimittelforschung. 1977;27(2b):463-6.
Base-induced condensation of alpha-mercapto-carboxylic esters with activated acetonitriles yields 2-methylene-thiazolidones-(4). The paper presented describes the development of ethyl (Z)-(3-ethyl-4-oxo-5-piperidino-thiazolidin-2-ylidene) acetate (30; piprozoline, Gö 919, Probilin), a novel choleretic with exocrin pancreas stimulating and hepatoprotective properties, by following-up the choleretic parent compound 2, which belongs to the 2-carbethoxymethylene-thiazolidones-(4) series. Synthesis and properties of piprozoline are reported. Structure-activity relationship is discussed in short.
碱催化α-巯基羧酸酯与活化乙腈缩合生成2-亚甲基噻唑烷酮-(4)。本文介绍了(Z)-(3-乙基-4-氧代-5-哌啶基-噻唑烷-2-亚基)乙酸乙酯(30;匹普唑啉、Gö 919、Probilin)的研发情况,它是一种新型利胆剂,具有刺激外分泌胰腺和保护肝脏的特性,其研发是基于对属于2-乙氧羰基亚甲基噻唑烷酮-(4)系列的利胆母体化合物2进行后续研究。文中报道了匹普唑啉的合成及性质,并简要讨论了构效关系。