Preparation method of Prucalopride intermediates

Abstract

The invention belongs to the field of medicine chemistry, and specifically relates to a preparation method of Prucalopride intermediates 1-(3-Methoxypropyl)-4-piperidinamine. The preparation method comprises following steps: dissolving 1-(3-Methoxypropyl)-4-piperidone (I) in an organic solvent, adding in saturated ammonia solution or ammonia salt and a reducing agent so as to obtain 1-(3-Methoxypropyl)-4-piperidinamine (II). The preparation method of Prucalopride intermediates has the advantages of simple operation, mild reaction conditions, high yield, and suitability for mass industry production.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and relates to a method for preparing 1-(3-methoxypropyl)-4-piperidinamine, an important intermediate of prucalopride (see I for the structure). [0002] [0003] I Background technique [0004] In recent years, with the impact of many factors such as living standards, lifestyles, and dietary structure, coupled with the rapid increase of the elderly population, the incidence of constipation in my country is on the rise. The huge consumer group of patients will strongly stimulate the continuous expansion of the constipation treatment drug market. [0005] Prucalopride is a selective 5-HT developed by Movetis NV in Belgium--------------------------------- ------------- 4 Receptor agonist, in October 2009, the European Medicines Agency approved the marketing of its monosuccinate, which is clinically used to treat female constipation that cannot be relieved by laxatives. For patients with va...

AI Technical Summary

Problems solved by technology

This article mainly involves the synthesis of 1-(3-methoxypropyl)-4-piperidinamine, an important intermediate of prucalopride. 3-methoxypropyl)-4-piperidone can be used as a raw material to prepare compound I by high-pressure hydrogenation, but this method uses palladium carbon and is expensive, and industrial hydrogenation has safety concerns. Improved, the improved method is easy to operate, the reaction conditions are mild, the yield is high, and it is suitable for large-scale industrial production

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