Photochemical C–H Arylation of Heteroarenes for DNA-Encoded Library Synthesis

DNA-encoded library (DEL) technology has emerged as a time- and cost-efficient technique for the identification of therapeutic candidates in the pharmaceutical industry. Although several reaction classes have been successfully validated...

Flow parallel synthesizer for multiplex synthesis of aryl diazonium libraries via efficient parameter screening

The development of miniaturized flow platforms would enable efficient and selective synthesis of drug and lead molecules by rapidly exploring synthetic methodologies and screening for optimal conditions, progress in which could be transformative for the field. In spite of tremendous advances made in continuous flow technology, these reported flow platforms are not devised to conduct many different reactions simultaneously. Herein, we report a metal-based flow parallel synthesizer that enables multiplex synthesis of libraries of compounds and efficient screening of parameters. This miniaturized synthesizer, equipped with a unique built-in flow distributor and n number of microreactors, can execute multiple types of reactions in parallel under diverse conditions, including photochemistry. Diazonium-based reactions are explored as a test case by distributing the reagent to 16 (n = 16) capillaries to which various building blocks are supplied for the chemistry library synthesis at the optimal conditions obtained by multiplex screening of 96 different reaction variables in reaction time, concentration, and product type. The proficiency of the flow parallel synthesizer is showcased by multiplex formation of various C–C, C–N, C–X, and C–S bonds, leading to optimization of 24 different aryl diazonium chemistries.

Unlocking the Potential of High-Throughput Experimentation for Electrochemistry with a Standardized Microscale Reactor

Organic electrochemistry has emerged as an enabling and sustainable technology in modern organic synthesis. Despite the recent renaissance of electrosynthesis, the broad adoption of electrochemistry in the synthetic community and, especially in industrial settings, has been hindered by the dearth of general, standardized platforms for high-throughput experimentation (HTE). Herein, we disclose the design of the HT<i>e^-</i>Chem, a high-throughput microscale electrochemical reactor that is compatible with existing HTE infrastructure, and enables rapid evaluation of a broad array of electrochemical reaction parameters. Utilizing the HT<i>e^-</i>Chem to accelerate reaction optimization, reaction discovery, and chemical library synthesis is illustrated using a suite of oxidative and reductive transformations under constant current, constant voltage, and electrophotochemical conditions.

Unlocking the Potential of High-Throughput Experimentation for Electrochemistry with a Standardized Microscale Reactor

Organic electrochemistry has emerged as an enabling and sustainable technology in modern organic synthesis. Despite the recent renaissance of electrosynthesis, the broad adoption of electrochemistry in the synthetic community and, especially in industrial settings, has been hindered by the dearth of general, standardized platforms for high-throughput experimentation (HTE). Herein, we disclose the design of the HT<i>e^-</i>Chem, a high-throughput microscale electrochemical reactor that is compatible with existing HTE infrastructure, and enables rapid evaluation of a broad array of electrochemical reaction parameters. Utilizing the HT<i>e^-</i>Chem to accelerate reaction optimization, reaction discovery, and chemical library synthesis is illustrated using a suite of oxidative and reductive transformations under constant current, constant voltage, and electrophotochemical conditions.

Unlocking the Potential of High-Throughput Experimentation for Electrochemistry with a Standardized Microscale Reactor

Organic electrochemistry has emerged as an enabling and sustainable technology in modern organic synthesis. Despite the recent renaissance of electrosynthesis, the broad adoption of electrochemistry in the synthetic community and, especially in industrial settings, has been hindered by the dearth of general, standardized platforms for high-throughput experimentation (HTE). Herein, we disclose the design of the HT<i>e^-</i>Chem, a high-throughput microscale electrochemical reactor that is compatible with existing HTE infrastructure, and enables rapid evaluation of a broad array of electrochemical reaction parameters. Utilizing the HT<i>e^-</i>Chem to accelerate reaction optimization, reaction discovery, and chemical library synthesis is illustrated using a suite of oxidative and reductive transformations under constant current, constant voltage, and electrophotochemical conditions.