We report an acridium-based organic photocatalyst as an efficient replacement for iridium-based photocatalysts to oxidise boronic acid derivatives by a single electron process. Furthermore, we applied the developed catalytic system to the synthesis of four active pharmaceutical ingredients (APIs). A straightforward scale up approach using continuous flow photoreactors is also reported affording gram an hour throughput.
We have devised a room temperature process for the cyclopropanation of electron-poor olefins using unstabilised diazo compounds, generated under continuous flow conditions. This protocol was applied to a wide range of different diazo species to generate functionalised cyclopropanes which are valuable 3D building blocks.
A continuous flow
method for the selective oxidation of secondary
alcohols is reported. The method is based on an Oppenauer-type ruthenium-catalyzed
hydrogen-transfer process that uses acetone as both solvent and oxidant.
The process utilizes a low loading (1 mol%) of the commercially available
ruthenium catalyst [Ru(p-cymene)Cl2]2 and triethylamine as a base and can be successfully applied
to a range of different substrates, with a good level of functional
group tolerance.
Afast, scalable, and safer C sp 3 ÀHoxidation of activated andu n-activated aliphatic chains can be enabled by methyl(trifluoromethyl)dioxirane (TFDO). The continuous flow platforma llows the in situ generation of TFDO gas and its rapid reactivity toward tertiarya nd benzylic Csp 3 ÀHb onds.T he process exhibits ab road scope and good functional groupc ompatibility ( 28 examples, 8-99 %). The scalability of this methodology is demonstrated on 2.5 gs cale oxidation of adamantane.
Pure pyrazinamide has been produced in a coupled flow synthesis and crystallisation in high yield, pure polymorphic form (γ) and narrow particle size distribution.
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