Accelerated drug discovery: A combinatorial diversity oriented flow synthesis approach

Drug discovery is exploring the chemical space aiming at finding chemicals which are able to interact with or regulate therapeutic biological targets1. However, development of an efficient and reliable synthetic method to produce a library of compounds which can represent a huge chemical space seems to be difficult and demanding. The present research aims at combining various synthetic strategies including diversity oriented synthesis, flow synthesis, combinatorial chemistry, multicomponent reactions and high throughput screening to suggest an accelerated method for sweeping and exploring the chemical space applicable to drug discovery.Combinatorial chemistry comprises chemical synthetic methods that make it possible to prepare a large number of compounds in a single process2. These compound libraries can be made as mixtures, sets of individual compounds or chemical structures generated by computer software. Flow chemistry, sometimes referred to as “continuous flow chemistry”, is the process of performing chemical reactions in a tube or pipe3. Reactive components are pumped together at a mixing junction and flowed down a temperature controlled pipe or tube. Using a narrow tube in flow synthesis offer the merits of laminar flow and microfluidic effects which facilitate catalytic reactions and separation of the products. Applying combinatorial, diversity oriented methods on multicomponent reactions in flow greatly accelerate and facilitate synthesis of a large array of diversified functionalized chemical structures which ameliorate drug discover technics offering a programmable, modular and efficient method for drug discovery.

Keywords:

Diversity oriented synthesis , Flow synthesis , Drug discovery , Combinatorial chemistry.