New Advances in Chemical Research, May 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic, and theoretical assessments of solvent structures and transition states. Formula: C9H5ClO2S, C9H5ClO2S. A document type is Patent, introducing its new discovery., Formula: C9H5ClO2S
The present invention relates to a process for the preparation of an amide from a carboxylic acid chloride and an organic molecule comprising both a primary amine group and a tertiary amine group, wherein the nitrogen atom of the tertiary amine group is comprised in a non-aromatic heterocycle and wherein the amide bond forms selectively with the primary amine group, comprising the step of reacting the carboxylic acid chloride with an organic molecule comprising both the primary amine group and the tertiary amine group, in the presence of imidazole. This is particularly useful in the preparation of amides from quinuclidin-3-amine, such as for the preparation of encenicline ((R) -7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide) from 7-chloro-benzo[b]thiophene-2-carboxylic acid chloride and (R)- quinuclidin-3-amine in the presence of imidazole. Encenicline is a nicotinic acetylcholine receptor agonist useful as a neuromodulator for the treatment of e.g. cognitive impairment, schizophrenia and Alzheimer’s disease.
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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem