Accessing New Chemical Entities through Microfluidic Systems

Abstract

Flow systems have been successfully utilized for a wide variety of applications in chemical research and development, including the miniaturization of (bio)analytical methods and synthetic (bio)organic chemistry. Currently, we are witnessing the growing use of microfluidic technologies for the discovery of new chemical entities. As a consequence, chemical biology and molecular medicine research are being reshaped by this technique. In this Minireview we portray the state-of-the-art, including the most recent advances in the application of microchip reactors as well as the micro- and mesoscale coil reactor-assisted synthesis of bioactive small molecules, and forecast the potential future use of this promising technology.

Chemical reaction engineering, process design and scale-up issues at the frontier of synthesis: Flow chemistry

“…Furthermore, a continuous flow system showed particularly effective and versatile for the synthesis of a new series of chemokine receptor ligands from commercial raw materials [63]. Other examples of newly developed molecules through continuous flow reactors are reviewed by Rodrigues et al [64].…”

Active Learning for Computational Chemogenomics

“…Put another way, the implication of our findings is that when models built by chemogenomic active learning on existing data are coupled with experimental screening platforms such that cycles of predicting, experimenting and model updating are iteratively performed, the potential reduction in experimental labor, time, and cost is large [99,100].…”

Picomole‐Scale Real‐Time Photoreaction Screening: Discovery of the Visible‐Light‐Promoted Dehydrogenation of Tetrahydroquinolines under Ambient Conditions

“…With this screening platform, we discovered an effective photocatalytic pathway involving the dehydrogenation of 1,2,3,4-tetrahydroquinolines to the corresponding quinolines. Surprisingly, the reaction was catalyzed by the common visible-light-harvesting complex [Ru-(bpy) 3 ]Cl 2 (bpy = 2,2'-bipyridine) under ambient conditions. The corresponding scaled up dehydrogenation reactions afforded the desired products in excellent yield in 2-4 h at ambient temperature, either under irradiation with an energysaving lamp or by exposure to sunlight.…”

“…However, most reaction systems involving transition-metal-based catalysts require long reaction times and moderately high temperatures (typically > 100 8C). Recently, a [Ru(phd) 3 ] 2+ /Co(salophen) cocatalyst system (phd = 1,10-phenanthroline-5,6-dione) was synthesized efficiently and found to promote the dehydrogenation of some tetrahydroquinolines to quinolines in relatively short reaction times (5-6 h) under ambient conditions.…”

“…Screening approaches [2] have become the mainstay of discovery processes to identify new chemical reactions and have increased the efficiency of reaction development. The use of microchannel reactors [3] is one of the most common approaches and provides an effective means of photoreaction screening. However, such studies usually require at least milligram (micromole) quantities of substrate per reaction, which may be a prohibitively large amount in preliminary reaction screening.…”