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Novel intermediate of medicine, and its preparation method

A compound and selected technology, applied in the preparation of sulfonate, organic chemistry, etc., can solve the problems of many unsafe factors, difficult to guarantee safety, and high cost

Active Publication Date: 2014-07-16
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are multiple methods for the synthesis of amlodipine reported in the prior art, such as patent applications WO2000024714, WO2007131759 and other reports to first synthesize the following formula (2), (3), (4), or the compound shown in (5), and then through reduction Or deprotection group obtains amlodipine, and its besylate salt can be obtained after salifying with benzenesulfonic acid; These methods have high cost, or because of using inflammable and explosive items such as azide or sodium hydride, unsafe factors are relatively There are many, so that the production requires high equipment and safety is difficult to guarantee; therefore, it is necessary to develop a process that is safe, simple in equipment requirements, and low in cost

Method used

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  • Novel intermediate of medicine, and its preparation method
  • Novel intermediate of medicine, and its preparation method
  • Novel intermediate of medicine, and its preparation method

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Embodiment Construction

[0009] In the first aspect, a novel intermediate for the synthesis of amlodipine or a pharmaceutically acceptable salt thereof is provided here, and the novel intermediate structure is shown in compound (03):

[0010]

[0011] Among them, R 2 , R 4 , R 5 , R 6 , R 7 Each independently selected from hydrogen, halogen.

[0012] In a second aspect, a process for the preparation of this novel intermediate compound (03) is provided herein.

[0013] The method for preparing compound (03) comprises: performing a nucleophilic substitution reaction between compound (01) and compound (02) to prepare compound (03), and the reaction formula is as follows:

[0014]

[0015] In compound (01) and compound (02), R 1 , R 3 each independently selected from a leaving group, and R 1 , R 3 At least one is hydroxyl; R in compound (02) 2 , R 4 , R 5 , R 6 , R 7 Same as defined in compound (03). In some embodiments, the leaving group is selected from halogen, hydroxyl, OSO 2 Me,...

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PUM

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Abstract

The invention relates to a novel intermediate and its preparation method. The intermediate can be used for preparing amlodipine or pharmaceutically acceptable salts thereof; and amlodipine or salts thereof can be prepared through preparing the intermediate. The method is simple and safe to operate, avoids the use of flammable and explosive articles, and is in favor of the industrial mass production.

Description

technical field [0001] The invention relates to a novel intermediate which can be used for preparing amlodipine or a pharmaceutically acceptable salt thereof and a preparation method of the novel intermediate. Background technique [0002] Amlodipine besylate has a structure as shown in formula (1), which is a calcium ion antagonist and can be used for treating hypertension and angina pectoris. There are multiple methods for the synthesis of amlodipine reported in the prior art, such as patent applications WO2000024714, WO2007131759 and other reports to first synthesize the following formula (2), (3), (4), or the compound shown in (5), and then through reduction Or deprotection group obtains amlodipine, and its besylate salt can be obtained after salifying with benzenesulfonic acid; These methods have high cost, or because of using inflammable and explosive items such as azide or sodium hydride, unsafe factors are relatively There are many, so that the production requires h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/90C07C309/29C07C303/32
CPCC07D211/90
Inventor 杜冲陈学明陈永好
Owner SUNSHINE LAKE PHARM CO LTD