Featured
-
-
News & Views |
Solid potential
Small-molecule drug discovery and development is limited by the ability of chemists to readily synthesize and purify new compounds with suitable chemical diversity. Now, a new twist on solid-phase chemical synthesis has enabled rapid and simplified synthesis of pharmaceutically relevant small molecules.
- Mark S. Kerr
- & Kevin P. Cole
-
Article |
Automated synthesis of prexasertib and derivatives enabled by continuous-flow solid-phase synthesis
Although strategies for the automated assembly of compounds of pharmaceutical relevance is a growing field of research, the synthesis of small-molecule pharmacophores remains a predominantly manual process. Now, an automated six-step synthesis of prexasertib is achieved by multistep solid-phase chemistry in a continuous-flow fashion using a chemical recipe file that enables automated scaffold modification through both early and late-stage diversification.
- Chenguang Liu
- , Jiaxun Xie
- & Jie Wu
-
Article |
Flow chemistry and polymer-supported pseudoenantiomeric acylating agents enable parallel kinetic resolution of chiral saturated N-heterocycles
Parallel kinetic resolution (PKR) of N-heterocycles via asymmetric acylation has been achieved using quasienantiomers of polymer supported hydroxamic acid reagents. Flow techniques provide physical separation of the reagents, establishing a practical implementation of PKR. The enantioenriched amide products can be readily deprotected to reveal the desired amine without detectable epimerization.
- Imants Kreituss
- & Jeffrey W. Bode
-
Article |
Iterative reactions of transient boronic acids enable sequential C–C bond formation
The ability to form multiple carbon–carbon bonds in a controlled sequence represents an important goal in modern chemical synthesis. Here, the in situ preparation of reactive allylic and benzylic boronic acids, obtained by reacting flow-generated diazo compounds with boronic acids, and their application in controlled iterative C–C bond forming reactions is described.
- Claudio Battilocchio
- , Florian Feist
- & Steven V. Ley
-
Review Article |
The past, present and potential for microfluidic reactor technology in chemical synthesis
The successes and failures of past research in the development of microfluidic reactors for chemical synthesis are highlighted. Current roadblocks are assessed and a series of challenges for the future of this area are identified.
- Katherine S. Elvira
- , Xavier Casadevall i Solvas
- & Andrew J. deMello
-
News & Views |
A light touch to a deadly problem
Flow chemistry has grown in stature as a technique with the potential to deliver synthetic complexity with assembly-line-like efficiency. Application of flow technology to the front-line antimalarial drug artemisinin promises to revolutionalize treatment.
- Kevin Booker-Milburn