Preparation method of 4-morpholino piperidine

By heating 1-benzyl-4-piperidone and morpholine in toluene solvent and performing subsequent treatment, combined with potassium carbonate and Pd/C catalysis, the yield and purity of 4-morpholinopiperidine were successfully improved. The problem of low product yield and purity in the existing technology is solved and is suitable for industrial production.

CN105777615AInactive Publication Date: 2016-07-20WUYAN PHARM TECH (SHANGHAI) CO LTD
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Patent Information

Application Number
CN201610212527.X
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2016-04-07
Publication Date
2016-07-20
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

The existing preparation method of 4-morpholinopiperidine has the problem of low product yield and purity, which affects the quality of pharmaceutical preparations.

Method used

1-benzyl-4-piperidone and morpholine are heated in a toluene solvent, and Raney nickel treated with absolute ethanol is added, and then filtered and treated with concentrated hydrochloric acid to obtain 4-(1-benzylpiperidine) -4-yl)morpholine dihydrochloride, then add potassium carbonate to tert-butanol to adjust the pH value, and use Pd/C to catalyze the reaction to prepare high-purity 4-morpholinopiperidine.

Benefits of technology

The yield and purity of the final product are significantly improved, the operation is simple, the reaction cycle is short, it is suitable for industrial production, and it has the advantages of safety and efficiency.

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Abstract

The invention relates to a preparation method of a drug intermediate, in particular to a preparation method of 4-morpholino piperidine.The preparation method comprises the steps that 1-benzyl-4-piperidone and morpholine are reacted to prepare 4-(1-benzyl piperidine-4-base) morpholine dihydrochloride, then, the reaction continues to be performed, and the end product 4-morpholino piperidine is obtained.The method is easy and convenient, the product yield and purity are high, the reaction condition is mild and high in safety, and the method is particularly suitable for industrial production.
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