Synthesizing method for N, N-double substitution-3-amino isoxazole-5-methanol compound

A technology for the synthesis of aminoisoxazoles and methods, which is applied in the field of synthesizing N,N-disubstituted-3-aminoisoxazole-5-methanol compounds, can solve the problems of long steps and harsh reaction conditions, and achieve mild reaction conditions , the reaction steps are simple, avoid the effect of catalyst
CN102558083AActive Publication Date: 2012-07-11WUXI BIOLOGICS CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
WUXI BIOLOGICS CO LTD
Publication Date
2012-07-11

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Abstract

The invention relates to a synthesizing method for an N, N-double substitution-3-amino isoxazole-5-methanol compound, and mainly solves the technical problems of long procedure, rigorous reaction conditions, toxic reagent using and the like in the conventional synthesis method. The synthesizing method for N, N-double substitution-3-amino isoxazole-5-methanol compound in the invention comprises the steps as follows: under the action of cesium fluoride, 3-bromine isoxazole-5-methenol 1 and an amine compound 2 are directly subjected to substitution reaction on a solvent-free condition to generate the N, N-double substitution-3-amino isoxazole-5-methanol compound 3. The reaction formula is as follows: the amine compound in one of pyrrolidine, piperidine and 4-methylpiperidine.
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Description

technical field

[0001] The invention relates to a synthetic N,N - Process for disubstituted-3-aminoisoxazole-5-methanol compounds. Background technique

[0002] Isoxazole derivatives are a class of compounds with medicinal value, and their derivatives have been used clinically as anti-arthritis drugs ( J. A. Clzn. Rheum. Dis. 1984 , 10, 385 . ), can also be used as a diuretic ( J. Indian Chem. Soc. 1946, 23 , 189.; Jpn. Kokai. Tokkyo Koho. JP79 14, 968 etc.) and precursors of pesticides ( Jpn. Kokai Tokkyo Koho JP 79 09,278), which has great development and utilization value in medicine and pesticides. As an important isoxazole derivative, 3-aminoisoxazole-5-methanol has attracted much attention in recent years due to its potential medicinal value ( PCT Int. Appl. , 2008036653). Unfortunately, only a small number of documents have reported its synthetic methods, and these methods have long synthetic steps, harsh reaction conditions, and use reagents such as hi...

Claims

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