Reactions of arylpropargyl amides of fumarate with a base by heating in xylenes under air gave benz[f]isoindolines. Heating the amides of fumarate and ethenetricarboxylate in DMSO gave aroyl-substituted pyrrolidines, probably via addition of water.
An in silico assay was designed, and generated compounds were studied to delimitate the synthesis by microwave irradiation–conventional heat combination. In vitro evaluation as antihyperglycemic and hypoglycemic agents were made, where 2s has good potential.
Synthesis and biological testing of the R- and S-enantiomers of LW223, a third generation TSPO PET imaging agent using human brain tissue showed that despite a 7.5-fold difference in affinity, both are insensitive to rs6971 polymorphism.
Proton and charge transfer rates in chemical ionisation are not solely association-limited. HiKE-IMS experiments and DFT modelling reveal how effective temperature, hydration, and intermediate barriers govern ionisation rate coefficients.
A new method for synthesizing 2-aminomethylpiperidine by selective hydrogenolysis of bio-renewable 2,5-bis(aminomethyl)furan was developed. The yield of 2-aminomethylpiperidine can reach 72% under mild conditions at 140 °C and 1 MPa H2 pressure.