1398705-01-5Relevant academic research and scientific papers
Development of a Continuous Flow Synthesis of 2-Substituted Azetines and 3-Substituted Azetidines by Using a Common Synthetic Precursor
Colella, Marco,Musci, Pantaleo,Cannillo, Debora,Spennacchio, Mauro,Aramini, Andrea,Degennaro, Leonardo,Luisi, Renzo
, p. 13943 - 13954 (2021)
The generation and functionalization, under continuous flow conditions, of two different lithiated four-membered aza-heterocycles is reported. N-Boc-3-iodoazetidine acts as a common synthetic platform for the genesis of C3-lithiated azetidine and C2-lithiated azetine depending on the lithiation agent. Flow technology enables easy handling of such lithiated intermediates at much higher temperatures compared to batch processing. Flow technology combined with cyclopentylmethyl ether as an environmentally responsible solvent allows us to address sustainability concerns.
Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors
Han, Younghue,Han, Minsoo,Shin, Dongyun,Song, Chiman,Hahn, Hoh-Gyu
, p. 8188 - 8192 (2012/11/07)
Novel azetidines based on the 3-aryl-3-oxypropylamine scaffold were designed, synthesized, and evaluated as TRIs. Reduction of 1 followed by Swern oxidation and then Grignard reaction gave 3. The alkylation of 3 provided the corresponding azetidine derivatives 6, of which the two most promising, 6bd and 6be, were selected from 86 prepared analogues based on their biological profiles. Compound 6be showed activity in vivo in FST at 10 mg/kg IV or 20-40 mg/kg PO.
