Scaling of the prospective anti-ulcer API synthesis
Journal Title: ScienceRise: Pharmaceutical Science - Year 2018, Vol 0, Issue 2
Abstract
<p><strong>Aim</strong>: the scaling of the laboratory procedure for the synthesis of 5-(4-methylphenylaminomethyl-4-(2-methylphenyl)-1,2,4-triazole-4H-3-ylthioacetic acid 4-methoxyanilide (Triazoprazole) for reproduction in industrial conditions.</p><p><strong>Methods.</strong> In the development of industrial technology, the efficiency of synthesis (yields at each stage of synthesis, the possibility of carrying out synthesis without isolation of some intermediates), compliance with the principles of green chemistry, and economic feasibility were evaluated. In accordance with the concept of Quality by design, the principles of green chemistry and previously developed algorithms for optimizing industrial synthesis, the theoretical possibilities of synthesis in industrial conditions were analyzed. The optimal reaction conditions are determined experimentally.</p><p><strong>Results.</strong> As a result of the experimental studies, the possibility of the synthesis of the key intermediate, 5-methylphenylaminomethyl-4- (2-methylphenyl) -1,2,4-triazole-3-thione, without isolation of the intermediate product, has been shown to increase its yield in terms of starting materials . The time for carrying out individual stages of synthesis has been shortened, and the yield and purity of the products remain appropriate. For the alkylation of the key intermediate, the reaction temperature is chosen as the optimum conditions-70 °C, the time is 1 hour, the use of the DMF-alkali system. Such conditions make it possible to ensure a high yield and purity of the final product.</p><p><strong>Conclusions</strong>: Scaling of the method of synthesis of a potential API with the antiulcer action of 5- (4-methylphenylaminomethyl-4- (2-methylphenyl) -1,2,4-triazole-4H-3-ylthioacetic acid 4-methoxyanilide for use in industrial production using Quality by design concept and "green chemistry"principles was carrying out, The number of stages of synthesis has been reduced and the conditions have been chosen in which the finished product is formed with the maximum yield and acceptable purity</p>
Authors and Affiliations
Narzullo Saidov
Keywords
Related Articles
- EP ID EP526818
- DOI 10.15587/2519-4852.2018.128885
- Views 213
- Downloads 0
Study of factors affecting on the development of the pharmaceutical sector enterprises
<p><strong>Aim. </strong>The aim of the article is to study the factors influencing the development of enterprises in the pharmaceutical sector.</p><p><strong>Materials and methods. </strong>Methods used in the study inc...
Development of method for quantitative analysis of corn silk for inclusion in the draft national monograph of the State Pharmacopoeia of Ukraine
<p>According to the concept of the development and implementation of monographs on herbal material to the State Pharmacopoeia of Ukraine, Corn silk is included into the list of herbal material which is described in the S...
Аналіз нормативно-правовового регулювання надання паліативної допомоги в Україні
<p><strong>Метою</strong> дослідження, результати якого наведено у статті, стало здійснення аналізу сучасного стану нормативно-правового регулювання паліативної допомоги в Україні.</p><p>У роботі використано<strong> мето...
Дослідження з вивчення ефективності антимікробних консервантів у розробці складу комбінованого сиропу
<p><strong>Мета:</strong> метою нашої роботи було обґрунтування та дослідження з вивчення ефективності антимікробних консервантів у розробці складу основи комбінованого сиропу на основі рослинної сировини, призначеного д...
Study of superoxide- and NO-dependent protective mechanisms of N-acetylcysteine and losartan in ratʼs aorta and liver under streptozoticin-induced type 1 diabetes mellitus
<p><strong>Aim.</strong> The aim of the research was to investigate superoxide- (SR) and NO-dependent mechanisms of action of N-acetylcysteine (NAC) and losartan (LOS) in aorta and liver of rats with type 1 diabetes mell...