Applications of the Combination of Microwave and Parallel Synthesis in Medicinal Chemistry

Abstract

The blending of microwave heating and parallel chemistry is a logical consequence of the significant rate enhancement and higher product yield afforded by microwave technology and the increase in productivity afforded by combinatorial chemistry. For this reason, this combination has become increasingly popular in the organic chemistry community. The current review highlights the application of this approach as a way to increase the rate of analogue synthesis in medicinal chemistry.

Novel Approach for Chemotype Hopping Based on Annotated Databases of Chemically Feasible Fragments and a Prospective Case Study: New Melanin Concentrating Hormone Antagonists

“…To prepare the target compounds in a fast and efficient way, microwave irradiation was used in an extensive way. 58 For the synthesis of target compound 30 (Scheme 2), cyclohexanol was used as protecting group. This group allowed us to hydrolyze selectively the chlorine atom and obtain pyrazinone 27.…”

Microwave-assisted synthesis of N-heterocycles in medicinal chemistry

“…Gupta showed an interest in discovering the nature of any combined effect of having both triazepine and triazole moieties in a single framework on the physiological activity. The work reported a mild and rapid procedure for the synthesis of 3,6diaryl-5H- [1,2,4]triazolo [4,3-b[1,2,4]triazepines from b-chlorocinnamaldehydes and 5-aryl-3,4-diamino-1,2,4-triazoles as outlined in Scheme 18. 45 The cyclisation was carried out under dielectric heating (domestic MW oven at 640 W) in DMF using p-TsOH as the catalyst.…”

“…Microwave-assisted organic synthesis in specially made equipment has grown into a mature technique that has been widely applied in the drug discovery eld, thanks to enhanced reaction rates, high yields, improved purity and greener reaction conditions. 1 The reader is referred to a series of recent general reviews [2][3][4][5] and monographs 6,7 for in-depth coverage of these subjects. Although readers are likely to be acquainted with the great potential of dielectric heating, the advantages and disadvantages of a particular device or the conditions needed to maximize the efficiency and functionality are oen overlooked.…”

Enabling technologies and green processes in cyclodextrin chemistry

“…Considering that MW ovens can be interfaced with autosamplers and that new MW reactors can accommodate multiple racks, this technique is well suited for fast optimization of organic protocols and parallel synthesis. The most impressive advantage of the MW technology is the appearance of the kilolab-scale reactors and their special versions that are operating in continuous flow mode [ 4 , 43 – 44 ].…”