Antitumor drug lenalidomide intermediate preparation method

An anti-tumor drug, the technology of lenalidomide, applied in the direction of organic chemistry, can solve the problems of low yield, unsatisfactory preparation, complex reaction, etc., to achieve simple and easy reaction, easy to obtain raw materials, and few reaction steps Effect
CN107488167AInactive Publication Date: 2017-12-19QINGDAO CHENDA BIOLOGICAL SCI & TECH

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
QINGDAO CHENDA BIOLOGICAL SCI & TECH
Publication Date
2017-12-19
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses an antitumor drug lenalidomide intermediate preparation method. The preparation method comprises the following steps: 1) under existence of cuprous iodide and organic alkali, performing contact reaction between 4-nitro indoline and 3-bromine-2,6-piperidine to obtain 3-(4-nitro-1,3-xylylenimine-2-yl)piperidine-2,6-diketone; 2) performing oxidizing reaction on the 3-(4-nitro-1,3-xylylenimine-2-yl)piperidine-2,6-diketone obtained in the step 1) to obtain lenalidomide intermediate of 3-(4-nitro-1-oxo-1,3-xylylenimine-2-yl)piperidine-2,6-diketone. The method disclosed by the invention has obviously smaller steps, the raw materials are easy to obtain, a yield is also improved, and the method is more suitable for industrial production.
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Description

technical field

[0001] The invention relates to the synthesis of drug intermediates, in particular to a method for preparing an anti-tumor drug lenalidomide intermediate. Background technique

[0002] Lenalidomide, the chemical name is 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)piperidine-2,6-dione, the drug mainly For the treatment of multiple myeloma bone marrow and dysplastic syndrome subtype diseases. Lenalidomide was developed by Celgene Biopharmaceutical Company of the United States. The application of lenalidomide in the treatment of multiple myeloma bone marrow and dysplastic syndrome subtype diseases has significantly improved the therapeutic effect of such diseases.

[0003] In the prior art, the preparation of lenalidomide is usually through the intermediate 3-(4-nitro-1-oxo-1,3-dihydroisoindol-2-yl)piperidine-2,6- Lenalidomide and lenalidomide intermediate 3-(4-nitro-1-oxo-1,3-dihydroisoindol-2-yl)piperidine-2,6 obtained by diketone reduction - Diketones are s...

Claims

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