A kind of synthetic method and product thereof of 2-aminoindane derivative

A synthesis method and aminoindan technology are applied in the preparation of aminohydroxy compounds, the preparation of amino compounds from amines, the preparation of carbon-based compounds, etc., and can solve the problems of difficult operation, cumbersome reaction steps, harsh reaction conditions and the like, and achieve easy operation, The effect of simple reaction steps and mild reaction conditions
CN105884626BActive Publication Date: 2017-10-20LONGXINING SHANGHAI PHARMA TECH CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
LONGXINING SHANGHAI PHARMA TECH CO LTD
Publication Date
2017-10-20

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Abstract

The invention provides a synthesis method of a 2-aminoindane derivative. According to the method, 5,6disubstituted 1-indanone is used as a staring raw material; bromination reaction is firstly performed; then, Gabriel reaction is performed; next, hydrazine hydrate is added; hydrolysis reaction is performed, and meanwhile, hydrazone is generated; finally, strong alkali is added into a high-boiling-point solvent to perform heating hydrolysis; the target product of the 2-aminoindane derivative is prepared. The invention also provides the 2-aminoindane derivative prepared by the synthesis method. Compared with the synthesis method of the 2-aminoindane derivative in the prior art, the synthesis method provided by the invention has the advantages that the reaction raw materials are cheap; the reaction condition is mild; the reaction steps are simple; the operation is easy; the yield of the obtained product is higher; the synthesis method is suitable for industrial production. Therefore good application prospects and market potentials are realized.
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Description

technical field

[0001] The invention belongs to the field of organic synthesis, and relates to a synthesis method of a pharmaceutical intermediate, in particular to a synthesis method of a 2-aminoindane derivative and a 2-aminoindane derivative product obtained by the synthesis method. Background technique

[0002] 2-aminoindan and its derivatives are common and widely used pharmaceutical intermediates, for example, 5,6-diethyl-2,3-dihydro-1H-inden-2-amine hydrochloride can be used It is used in the synthesis of β2 adrenoceptor agonists for indications such as asthma and chronic obstructive pulmonary disease; as another example, the antihypertensive drug delapril and the antiarrhythmic drug ambroxidine are used in their respective preparation processes. to 2-aminoindan; in addition, EP1018514A1 discloses an indane derivative used as an NF-KB inhibitor, etc.

[0003] Also provide some synthetic methods of 2-aminoindane derivatives in the prior art, as EP1018514A1 provides a ...

Claims

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