Method for preparing 5-(N,N-dibenzylglycyl) salicylamide

A technology of dibenzylaminoacetyl and acetylsalicylic amide, applied in the field of preparation of 5-salicylic amide, can solve problems such as inability to satisfy, and achieve the effects of low product cost, convenient and abundant sources, and low impurity content
CN101560171AInactive Publication Date: 2009-10-21JIANDE ZISHANWAN FINE CHEM
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
JIANDE ZISHANWAN FINE CHEM
Publication Date
2009-10-21
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention belongs to the field of medical intermediate, and particularly discloses a method for preparing a 5-(N,N-dibenzylglycyl) salicylamide. The method comprises the following steps of mixing dibenzylamine and 5-(bromoacetyl) salicylamide with the molar ratio more than or equal to 2 and taking carbinol and water as solvent so as to react under the circumfluence condition at the temperature less than or equal to 40 DEG C; obtaining a coarse product by centrifuging the reaction products, and refining the coarse product by ethyl acetate, thus obtaining the 5-(N,N-dibenzylglycyl) salicylamide. The method has the advantages of simple preparation method, easy industrial production, high product yield, high purity, etc.
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Description

technical field

[0001] The invention relates to the field of pharmaceutical intermediates, in particular to a preparation method of 5-(N,N-dibenzylaminoacetyl) salicylamide. Background technique

[0002] 5-(N,N-dibenzylaminoacetyl) salicylamide is an important intermediate in the manufacture of cardiovascular drug labetalol hydrochloride (saladol).

[0003] Labetalol hydrochloride is an antihypertensive drug with α and β receptor blocking effects. It is the first representative drug that simultaneously blocks α and β receptors in clinical application. It has become one of the antihypertensive drugs widely used in European and American countries because of its strong and definite curative effect. Once the drug came out, it was rapidly promoted in countries all over the world. The drug is suitable for all kinds of high blood pressure, especially safe and effective for hypertensive crisis. It is also suitable for high blood pressure with coronary heart disease and high blood p...

Claims

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