Herein we report a convenient, fast, and high-yielding method for the generation of the racemic amide anaesthetics mepivacaine, ropivacaine, and bupivacaine. Coupling of α-picolinic acid and 2,6-xylidine under sealed-vessel microwave conditions generates the intermediate amide after a reaction time of only 5 min at 150°C. Subsequent reaction in a continu-
An efficient three-step protocol was developed to produce 2-(azidomethyl)oxazoles from vinyl azides in a continuous-flow process. The general synthetic strategy involves a thermolysis of vinyl azides to generate azirines, which react with bromoacetyl bromide to provide 2-(bromomethyl)oxazoles. The latter compounds are versatile building blocks for nucleophilic displacement reactions as demonstrated by their subsequent treatment with NaN3 in aqueous medium to give azido oxazoles in good selectivity. Process integration enabled the synthesis of this useful moiety in short overall residence times (7 to 9 min) and in good overall yields.
(R)‐Propylene carbonate is an important intermediate in the synthesis of tenofovir pro‐drugs such as tenofovir alafenamide fumarate (TAF) and tenofovir diisoproyl fumarate (TDF). Independent of the pro‐drug type, tenofovir presents a chiral secondary hydroxy derivative, which can be obtained directly from (R)‐propylene carbonate. Herein, we report our chemo‐enzymatic continuous‐flow strategy towards (R)‐propylene carbonate starting from a very cheap and renewable raw material, glycerol. We were able to synthesize (R)‐propylene carbonate in seven continuous‐flow steps, starting from glycerol, in good‐to‐excellent yields (66–93 %) and excellent selectivity (E > 200).
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