3797-94-2Relevant articles and documents
Sodiation of Arenes and Heteroarenes in Continuous Flow
Weidmann, Niels,Ketels, Marthe,Knochel, Paul
supporting information, p. 10748 - 10751 (2018/07/30)
The first sodiations of (hetero)arenes in continuous flow using NaDA (sodium diisopropylamide) in Me2EtN are reported. This flow procedure enables sodiation of functionalized arenes and heteroarenes that decompose under batch-sodiation conditions. The resulting sodiated (hetero)arenes react instantly with various electrophiles, such as ketones, aldehydes, isocyanates, alkyl bromides, and disulfides, affording polyfunctionalized (hetero)arenes in high yields. Scale-up is possible without further optimization.
Continuous flow photochemistry as an enabling synthetic technology: Synthesis of substituted-6(5: H)-phenanthridinones for use as poly(ADP-ribose) polymerase inhibitors
Fang,Tranmer
supporting information, p. 720 - 724 (2016/05/19)
Methods utilizing continuous flow photochemistry, an enabling synthetic technology, have been developed for the generation of phenanthridinones via an intramolecular photochemical cyclization of 2-chlorobenzamides for the purposes of generating poly(ADP-ribose) polymerase inhibitors. Herein we report 16 examples of a single-step flow photocyclization which produces substituted phenanthridinones in yields up to 99%, while a two-step method leads directly to phenanthridinones from 2-chlorobenzoyl chlorides and anilines via a novel continuous flow amidation/photocyclization protocol. Overall, the flow photocyclization reactions typically progress in good to excellent yields, and in a superior fashion to analogous batch methods, greatly enabling the drug discovery process.
Diacylamines - Perfect Acylating Agents for Peptide Synthesis
Gruszecki, Wojciech,Gruszecka, Maria,Bradaczek, Hans
, p. 331 - 336 (2007/10/02)
A new series of diacylamines containing N-protected amino acids have been synthesized.These diacylamines, possessing ortho-substituted benzoyl groups were found to be excellent acylating agents for peptide synthesis.In this reaction the 2,6-dichlorobenzoy