The esterification reaction of chitin with perflurocarboxylic acid was studied in methanic acid or perfluorocarboxylic acid as solvent. A series of substituted derivatives of trifluoroacyl. perfluorobutyric and perfluorooctanoyl chitin were synthesized. The properties of these chitin derivatives were investigated.
The Front Cover shows the therapeutic effect of the H3 receptor inverse agonist LML134 (18b), as expected in narcoleptic patients. Compound 18b results from an extensive optimization of safety and pharmacokinetic properties of several chemical series. It was selected for its ability to achieve high receptor occupancy in the brain within a short time frame, followed by fast target disengagement. This profile was designed to increase wakefulness during the day and help re‐establish a normal sleep pattern, without the risk of mechanism‐related insomnia during the night following drug administration. Compound 18b completed Phase I studies, and is undergoing further clinical trials to confirm its wakefulness‐promoting effect in patients suffering from shift‐work disorder. More information can be found in the Full Paper by Yves P. Auberson et al. on page 1238 in Issue 13, 2019 (DOI: 10.1002/cmdc.201900176).
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.