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Preparation method of ketone drug intermediate

A technology for intermediates and drugs is applied in the field of preparation of ketone drug intermediates, which can solve the problems that the reaction process is not meaningful for reference, and achieve the effects of simple preparation process, high yield and purity.

Inactive Publication Date: 2014-05-14
WUXI VISION PRO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, in the prior art, specific reaction process routes are adopted for specific pharmaceutical intermediates. For different intermediates, the reaction process is of little reference value.

Method used

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  • Preparation method of ketone drug intermediate

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Embodiment 1

[0014] A preparation method of a ketone drug intermediate, the ketone drug intermediate is 1-isopropyl-4,6-dihydrospiro[indazole-5,4'-piperidine]-7(1H)- Ketones, the steps of which include:

[0015] 250 g of tert-butyl 9-oxo-3-azaspiro[5.5]undec-7-ene-3-carboxylate and 325 ml of tris(dimethylaminomethane) were dissolved in 1.9 liters of toluene and heated under reflux 4 hours. The mixture was distilled and concentrated to a minimum stirred volume at 110° C., then 1.9 liters of toluene were added. The reaction was redistilled to a minimum stirred volume and cooled to room temperature. 1.8 liters of toluene and 135 grams of prohydrazine hydrochloride were added and the solution was heated to reflux for 5 hours. The reaction was cooled to room temperature and then washed with 150 mL of 10% aqueous citric acid and 200 mL of water, and the organic layer was then distilled to a minimum stirring volume. 2 liters of methanol were added and distilled to a minimum stirred volume. T...

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Abstract

The invention discloses a preparation method of a ketone drug intermediate. The prepared ketone compound can be used for preparing a drug for treating obesity. According to the preparation method disclosed by the invention, the preparation process is simple, and the yield and purity are both relatively high. The ketone drug intermediate can be directly applied after little further treatment.

Description

technical field [0001] The invention relates to a preparation method of a drug intermediate, in particular to a preparation method of a ketone drug intermediate. Background technique [0002] The so-called pharmaceutical intermediates, or pharmaceutical intermediates, are actually some chemical raw materials or chemical products used in the process of pharmaceutical synthesis. This kind of chemical product does not require a drug production license, and can be produced in ordinary chemical factories. As long as it reaches a certain level, it can be used in the synthesis of drugs. [0003] Among pharmaceutical intermediates, ketone pharmaceutical intermediates are a very important class of pharmaceutical intermediates, and their preparation process is also the focus of research and development in the technical field. [0004] CN 102070514A discloses a preparation method of a hemosanone intermediate, which includes the following steps: step (1) adding a solution of compound F...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/10
CPCC07D471/10
Inventor 廖秀高
Owner WUXI VISION PRO