Synthesis method of 6-(trifluoromethyl) isoquinoline-5-ol

A technology of trifluoromethyl isoquinoline and trifluoromethyl, which is applied in the field of synthesis of 6-(trifluoromethyl) isoquinoline-5-ol, can solve problems such as incapability of large-scale production, and achieve easy The effect of amplification, reasonable process selection and low cost of raw materials

Active Publication Date: 2020-12-18
SUZHOU KANGRUN PHARMA
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Problems solved by technology

[0003] At this stage, there is no published synthetic route of 6-(trifluoromethyl)isoquinolin-5-ol. At present, the main synthetic method of 6-trifluoromethylisoquinoline is to pass p-benzylamine under microwave Condensation reaction and sulfuri

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  • Synthesis method of 6-(trifluoromethyl) isoquinoline-5-ol

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[0041] The present invention will be further described below in conjunction with specific examples, but the examples are only exemplary and do not constitute any limitation to the scope of the present invention. Those skilled in the art should understand that the details and forms of the technical solutions of the present invention can be modified or replaced without departing from the spirit and scope of the present invention, but these modifications and replacements all fall within the protection scope of the present invention.

[0042] The synthesis process of 6-(trifluoromethyl)isoquinolin-5-amine of the present invention is based on the raw material of m-trifluoromethylphenethylamine, and undergoes amino protection, ring closure, hydrolysis, bromination and debromination of alkenes with TFAA. and dehydroaromatization to obtain 7-trifluoromethylisoquinoline, and NBS for 5-bromination to generate 5-bromo-7-trifluoromethylisoquinoline, methoxylation and demethylation with sodium m

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Abstract

The invention discloses a synthesis method of 6- (trifluoromethyl) isoquinoline-5-ol, which comprises the following steps of by using p-trifluoromethyl phenylethylamine as a raw material, carrying outamino protection, cyclization, hydrolysis, bromination, debromination alkene insertion and dehydroaromatization on the p-trifluoromethyl phenylethylamine and TFAA to obtain 7-trifluoromethyl isoquinoline, and carrying out 5-site bromination on the 7-trifluoromethyl isoquinoline and NBS to generate 5-bromine- 7-trifluoromethyl isoquinoline, and carrying out methoxylation and demethylation with sodium methoxide to obtain 6-(trifluoromethyl) isoquinoline-5-alcohol. The method is simple in synthetic route, reasonable in process selection, low in raw material cost, simple and easily available in raw materials, convenient to operate and post-treat, high in total yield, free of highly toxic reagents and easy to amplify, and can be used for large-scale production.

Description

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Claims

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Application Information

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Owner SUZHOU KANGRUN PHARMA
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