Uniqsis has announced that researchers at Lilly S.A have developed a novel continuous flow approach for the Wadsworth–Emmons cyclopropanation of alkyl-substituted chiral epoxides into chiral cyclopropane carboxylic acids.
Employing a FlowSyn continuous flow reactor and binary pump in a custom set-up, the team developed a new flow process which circumvented the risks associated with high temperature and pressure requirements, and the highly volatile nature of the epoxide starting material.
The FlowSyn flow reactor additionally offered increased efficiency, as its reduced headspace contributes to keeping a higher concentration of the low-boiling-point reactants in the liquid phase; thus enhancing reactivity, contrary to the use of sealed vessels in batch.
The researchers coupled their cyclopropane formation process with in-line workup and hydrolysis transformations to yield the desired enantiomerically pure cyclopropane carboxylic acids in good yields up to the 100 g scale.
Designed by Uniqsis’s team of experienced flow chemists and engineers - FlowSyn is a fully integrated, easy to use continuous flow reactor for seamless reaction optimisation and scale up from milligrams to 100s of grams. For further information about the FlowSyn continuous flow reactor please visit https://www.uniqsis.com/paFlowSystem.aspx or contact Uniqsis now on +44-1223-942004 / info@uniqsis.com.
Since 2007, Uniqsis has specialised in the design and supply of mesoscale continuous flow chemistry systems for a wide range of applications in chemical and pharmaceutical research. The company’s aim is to make flow chemistry easily accessible to both novices and experienced users.
Reference:
https://pubs.acs.org/doi/10.1021/acs.oprd.3c00444#
