Awesome Chemistry Experiments For 123536-14-1

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PROCESS FOR THE PREPARATION OF ENCENICLINE FROM 7-CHLORO-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID CHLORIDE AND (R)-QUINUCLIDIN-3-AMINE IN THE PRESENCE OF IMIDAZOLE

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.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Safety of (R)-3-Aminoquinuclidine dihydrochloride, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about Safety of (R)-3-Aminoquinuclidine dihydrochloride

Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H116N | ChemSpider