222960-38-5Relevant academic research and scientific papers
Novel approach to the synthesis of istaroxime
Liang,Guo,Jiang
, p. 2643 - 2647 (2017/12/26)
Istaroxime 1, a novel cardiotonic agent with high efficiency and low toxicity was synthesized from dehydroepiandrosterone 2 using a novel approach that included epoxidation, ring-opening, substitution, and oximation. The new protocol without gas protection was milder than the reported approaches. The overall yield of the method was 24.1%.
Novel synthesis method of Istaroxime
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Paragraph 0123; 0124; 0125; 0126; 0127-0130; 0169, (2016/10/10)
The invention belongs to the field of pharmaceutical chemistry, and discloses a novel synthesis method of Istaroxime. The method comprises the following steps: by using dehydrogenated epiandrosterone as an initial raw material, carrying out epoxidation, ring opening, reduction, oxidation and other reactions to prepare an intermediate M-06; by using ethyl benzoate as an initial raw material, reacting the ethyl benzoate with hydroxylamine hydrochloride to obtain phenyl hydroximic acid, carrying out hydrochlorination and chlorination by using ethanolamine as a raw material to obtain dichloroacetate, and carrying out substitution, hydrolysis and other reactions on the dichloroacetate and the phenyl hydroximic acid to obtain an intermediate M-11; and finally, reacting the M-06 with the M-11 to obtain the end product Istaroxime. According to the method, in the intermediate M-06 synthesis process, the polarity of all the intermediates has great differences from that of the impurities and reaction reagents; and in the intermediate 11 synthesis process, the active spots capable of participating in the chemical reaction in the reaction substrate are simple. Therefore, the method can achieve the requirements without carrying out column chromatography purification, thereby simplifying the synthesis after-treatment process.
AN IMPROVED SYNTHETIC ROUTE TO AMONOXYPROPYLAMINE (APA) AND RELATED HOMOLOGS
Pankaskie, Marvin C.,Scholtz, Stephen A.
, p. 339 - 344 (2007/10/02)
Aminoxypropylamine (APA) has been found to be a potent inhibitor of several enzymatic pathways involved in the biosynthesis of the naturally occuring polyamines putrescine, spermidine, and spermine.This report describes a convenient, three-step synthesis of APA, as well as its ethyl and butyl homologs, utilizing starting materials and intermediates useful in the preparation of other related aminoxyalkylamines.
