Green environment-friendly synthetic method for mosapride citrate

Abstract

The invention discloses a green environment-friendly synthetic method for mosapride citrate and relates to the technical field of organic synthesis. The method comprises the following steps: by taking 2-aminomethyl morpholine as a raw material, performing condensation reaction on the 2-aminomethyl morpholine and 5-chlorine-4-amino-2-ethyoxyl benzoic acid, thereby acquiring a midbody (C); utilizing acetic anhydride to protect an amino group on benzene ring of the midbody (C), thereby acquiring a midbody (D); performing alkylation reaction on the midbody (D) and fluorobenzyl chloride in the presence of inorganic alkali, thereby acquiring a midbody (E); hydrolyzing amino protection group of the midbody (E) in a citric acid aqueous solution and salifying with citric acid, thereby acquiring a crude product of mosapride citrate; and refining the crude product of mosapride citrate with ethyl alcohol, thereby acquiring a pure product of mosapride citrate. According to the invention, the low-cost easily acquired 2-aminomethyl morpholine is used for directly introducing morpholine group, so that the output of three wastes is obviously reduced, the use rate of the equipment is increased and the purpose of green environment-friendly production is achieved.

Description

Technical field: [0001] The invention relates to the technical field of organic synthesis, in particular to a green and environment-friendly synthesis method of mosapride citrate. Background technique: [0002] Mosapride citrate is mainly used for functional dyspepsia with heartburn, belching, nausea, vomiting, early satiety, upper abdominal distension and other gastrointestinal symptoms. Mosapride citrate is a selective 5-hydroxytryptamine 4 (5-HT4) receptor agonist, which promotes the production of acetylcholine by exciting the 5-HT4 receptors of cholinergic interneurons and myenteric plexuses in the gastrointestinal tract. release, thereby enhancing the motility of the gastrointestinal tract, improving the gastrointestinal symptoms of patients with functional dyspepsia, without affecting the secretion of gastric acid. [0003] [0004] The existing synthesis method of mosapride citrate is cumbersome, and the three wastes are seriously polluted. When producing the impo...

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Problems solved by technology

[0004] The existing synthesis method of mosapride citrate is cumbersome, and the pollution of three wastes is serious. When producing important intermediate A, epichlorohydrin is used as the introduction agent, and then a large amount of concentrated sulfuric acid is used to close the ring. The purity of the obtained crude product is very low, and it must be Use acetic anhydride to protect and acylate the amino group to obtain the acetylated product as a means of purification, and then hydrolyze the acetylated product to obtain intermediate A

The entire process of synthesizing intermediate A is lengthy and produces a large amount of waste residue and concentrated acid wastewater, the utilization rate of equipment is also very low, and the manufacturing cost is huge, which is inconsistent with the current social situation of clean production

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