Preparation method of (3-(3-(dimethylamino) propoxy) phenyl) boronic acid

A technology of dimethylaminochloropropane and dimethylamino, which is applied in the field of preparation of propoxy)phenyl)boronic acid, can solve problems such as unsuitable for scale-up production, harsh reaction conditions, and high risk of reagents, and meets the reaction conditions and is easy Control, ease of purification, and ease of operation
CN107188901AInactive Publication Date: 2017-09-22CHEMSHUTTLE
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Patent Information

Authority / Receiving Office
CN Β· China
Current Assignee / Owner
CHEMSHUTTLE
Publication Date
2017-09-22
Estimated Expiration
Not applicable Β· inactive patent

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Abstract

The invention discloses a preparation method of (3-(3-(dimethylamino) propoxy) phenyl) boronic acid. The preparation method comprises the following steps: (1) with 3-hydroxybenzeneboronic acid as a starting material, performing an esterification reaction to obtain 3-hydroxybenzeneboronic pinacol ester; (2) then, coupling the 3-hydroxybenzeneboronic acid pinacol ester with N, N-dimethylaminopropane hydrochloride to obtain (3-(3-(dimethylamino) propoxy) phenyl) boronic acid pinacol ester; (3) finally, hydrolyzing the (3-(3-(dimethylamino) propoxy) phenyl) boronic acid pinacol ester to obtain the (3-(3-(dimethylamino) propoxy) phenyl) boronic acid. The preparation method is short in process route, easy to operate, mild in reaction condition, easy to control and low in cost; by the preparation method, industrialization is easily realized, use of an expensive catalyst and use of metal alkali with relatively high danger are avoided, purification is easy and the yield rate is relatively high.
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Description

Technical field

[0001] The present invention relates to the technical field of the synthesis of pharmaceutical intermediates, in particular to a preparation of 3-(3-(dimethylamino)propoxy) using 3-hydroxyphenylboronic acid as a raw material through the process of esterification, coupling and hydrolysis. Phenyl) boric acid method. Background technique

[0002] The introduction of dimethylamine into organic compounds is water-soluble, which can promote the absorption and delivery of drugs in the body. In the existing drugs, a large number of structures containing dimethylamino can be seen.

[0003] Aryl boronic acid is a kind of organic synthesis, pharmaceutical and chemical intermediates that are relatively stable in the air, are not sensitive to moisture, can be stored for a long time, and have high reactivity. The Suzuki coupling reaction of aryl boronic acid and halogenated aromatic hydrocarbon has good position and stereo selectivity. Various chemical functional groups do not c...

Claims

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