Method for preparing Prasugrel intermediate alpha-cyclopropylcarbonyl-2-fluorobenzyl bromide

A technology of cyclopropylcarbonyl and fluorobenzyl, which is applied in the field of preparation of prasugrel intermediate α-cyclopropylcarbonyl-2-fluorobenzyl bromide, can solve the problems of safe operation, environmental protection, unfavorable economy and product purity Not high, bromine is not easy to recycle, etc.

Active Publication Date: 2011-09-21
ZHEJIANG HISOAR PHARMA +1
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Problems solved by technology

In the disclosed patents at present, the preparation of α-cyclopropylcarbonyl-2-fluorobenzyl bromide all adopts bromine or N-bromosuccinimide (NBS) as the bromination reagent, and bromine will produce a large amount of Hydrobromic acid, while NBS also uses bromine in the process of recovery and reuse. At the same time, i

Method used

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  • Method for preparing Prasugrel intermediate alpha-cyclopropylcarbonyl-2-fluorobenzyl bromide
  • Method for preparing Prasugrel intermediate alpha-cyclopropylcarbonyl-2-fluorobenzyl bromide
  • Method for preparing Prasugrel intermediate alpha-cyclopropylcarbonyl-2-fluorobenzyl bromide

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Abstract

The invention discloses a new method for preparing a Prasugrel intermediate alpha-cyclopropylcarbonyl-2-fluorobenzyl bromide which is a compound shown as a formula (III). In the method, a compound shown as a formula (I), namely cyclopropyl-2-fluorobenzyl ketone is taken as a raw material, and is bromized by a compound show as a formula (II), namely phenyltrimethylammonium tribromide to form the target product of alpha-cyclopropylcarbonyl-2-fluorobenzyl bromide, namely the compound in the formula (III). The method has the advantages of mild reaction conditions, high selectivity, high yield, low cost and environmental friendliness, and is suitable for large-scale industrial production.

Description

Method for preparing prasugrel intermediate α-cyclopropylcarbonyl-2-fluorobenzyl bromide Technical field The invention belongs to the field of medicine and chemical industry, and specifically relates to a preparation method of prasugrel intermediate α-cyclopropylcarbonyl-2-fluorobenzyl bromide. Background technique Prasugrel is a tetrahydrothienopyridine compound similar to clopidogrel. It has the advantages of platelet aggregation inhibitory effect, good oral absorption, strong metabolic activity and weak toxicity. Clinical Phase III shows superior activity, tolerability and safety than clopidogrel, so it is a promising antithrombotic drug. At present, the preparation methods of prasugrel mainly include EP192535, EP542411, US4740510, US5288726, US5874581, WO04098713, CN101250193, CN92111584, CN10117743, etc. Among all the disclosed methods, α-cyclopropylcarbonyl-2-fluorobenzyl bromide (formula III) is an important intermediate indispensable for the preparation of prasugrel. ...

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Application Information

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IPC IPC(8): C07C49/567C07C45/63
Inventor 王立新周勇徐小英唐鹤黄青春蒋君慧
Owner ZHEJIANG HISOAR PHARMA
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