Preparation method of urapidil intermediate 1-(2-methoxyphenyl) piperazine and salt thereof

A technology of methoxyphenyl and urapidil, which is applied in the field of preparation of urapidil intermediate 1-piperazine and its salt, can solve the problems of low yield, heavy metal residue, high cost of raw materials, etc., and improve product purity , easy operation, guaranteed selective effect
CN114685399APending Publication Date: 2022-07-01河北广祥制药有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
河北广祥制药有限公司
Publication Date
2022-07-01

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Abstract

The invention belongs to the field of organic synthesis, and particularly relates to a preparation method of urapidil intermediate 1-(2-methoxyphenyl) piperazine and salt thereof. According to the invention, o-methoxyphenol is used as a starting material to prepare the urapidil intermediate 1-(2-methoxyphenyl) piperazine by using a brand-new synthesis route, and methylsulfonyl chloride is adopted to activate hydroxyl on o-methoxyphenol, so that the condensation reaction condition of o-methoxyphenol and imino on piperazine is mild; and the intermediate product does not need to be separated in the intermediate process of the sulfonylation reaction and the condensation reaction, and the operation is simple and convenient. The condensation reaction adopts a mode of adding o-methoxyphenyl methanesulfonate into piperazine, so that two imino groups on piperazine are prevented from being subjected to condensation reaction at the same time, the selectivity of a target product is ensured, excessive impurities are prevented from being introduced into a system, and the purity of the product is improved. In terms of o-methoxyphenol, the total yield of the urapidil intermediate 1-(2-methoxyphenyl) piperazine prepared by the preparation method disclosed by the invention can reach 88% or above. Meanwhile, the preparation method is obvious in cost advantage and suitable for industrial production.
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Description

technical field

[0001] The invention belongs to the field of organic synthesis, in particular to a preparation method of a urapidil intermediate 1-(2-methoxyphenyl)piperazine and a salt thereof. Background technique

[0002] Urapidil is an alpha-adrenergic receptor blocker. As a new type of antihypertensive drug, since it entered the clinic in the 1970s, it has been increasingly used in clinical practice with its unique blood pressure lowering mechanism and significant blood pressure lowering effect. 's approval. Urapidil not only has no significant effect on biochemical indicators such as blood glucose, blood lipids, uric acid, liver function, blood urea nitrogen and creatinine, but also has no significant effect on the patient's heart rate. Patients with gout can take it. At the same time, urapidil also has the functions of increasing high-density lipoprotein, lowering cholesterol, reversing left ventricular hypertrophy and reducing insulin resistance. Therefore, urapidil...

Claims

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