|
Author
Broto Fantova, Anna
|
Abstract
In the last several years, functionalized pyrido[2,3-d]pyrimidine derivatives have gained relevance by dint of their great pharmacological activity, for instance, antitumor, antibacterial, anti-inflammatory, antimicrobial and kinase inhibitor. In order to obtain these derivatives, the essential intermediate products are 4,5-substituted 2-methoxy-6-oxo-1,4,5,6-tetrahydropyridine-3-carbonitriles which are achieved by means of a cyclic strategy. As a means of automating the process of obtention, reducing reaction time and enhancing quality, among others, flow chemistry was used to acquire 2-methoxy-6-oxo-1,4,5,6-tetrahydropyridin-3-carbonitriles.
Moreover, when synthesizing a compound, the highest value of yield is searched to obtain the maximum quantity of product using the minimum amount of reagents and solvents. In this way, the use of design of experiments methodology in pharmaceutical processes, has considerable increased over the last years as it is a powerful tool that allows to determine the optimum values for a certain chemical process. These optimum values can be related to parameters as temperature, pressure, reaction time, etc. So, in order to optimize the obtention process, this tool was applied to the synthesis of 4,5-substituted 2-methoxy-6-oxo-1,4,5,6-tetrahydropyridin-3-carbonitriles via continuous flow chemistry.
On the other hand, aryl halides are building blocks in organic chemistry for the synthesis of many complex structures. These aryl halides can be found in natural products, however, as their availability depends on the halide bounded to the benzene, they are obtained via Finkelstein and retro-Finkelstein reactions. In addition, the principal limitation of this process is the reaction time. Thusly, as the reaction is catalysed by copper, in order to reduce the reaction time this synthesis was carried out by means of continuous flow chemistry with a copper reactor.
|
|
