Preparation method of 2-cyclopropyl ethylamine

Abstract

The invention discloses a preparation method of 2-cyclopropyl ethylamine. The method includes the steps of A, compound 1 and nitromethane react under the action of alkali to obtain compound 2; B, the compound 2 is dehydrated under the action of dehydration reagent to obtain compound 3; C, the compound 3 reacts in solvent under the action of reducing agent to obtain compound 4; D, the compound 4 reacts under the action of reduction hydrogenation catalyst to obtain compound 5, namely the 2-cyclopropyl ethylamine. The preparation method has the advantages that operation conditions can be simplified, cost can be lowered, and easiness in large batch production is achieved. The synthesizing route is showed as follows.

Description

technical field [0001] The invention relates to a preparation method of 2-cyclopropylethylamine. Background technique [0002] 2-Cyclopropylethylamine is an aliphatic amine containing a three-membered ring. It is an important pharmaceutical intermediate and fine chemical intermediate, and is widely used in the fields of medicine, pesticides and organic synthesis. At present, little work has been done on the development and application of 2-cyclopropylethylamine in China, and its output is far from meeting the market demand. There are not many reports on the synthesis of 2-cyclopropylethylamine so far. Among them, Kuraray Co., Ltd disclosed a related patent document EP1445248 A1. EP1445248 A1 has reported the synthesis of this compound, and route is as follows: [0003] . [0004] However, in the above synthetic route, every step of the reaction must be purified by column chromatography, and the route has low yield, poor reaction repeatability, unstable yield, and is n...

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Problems solved by technology

[0007] This method also has the disadvantage of low yield (the total yield is less than 5%), and it is difficult to apply it on a large scale

[0008] In addition, the literature published in Journal of Medicinal Chemistry, 1998, vol.41, #18.p.3515–3529, International Patent Application WO2006 / 34338 A1 and Tetrahedron , 2014, vol.70, # 4 p.975-983, the documents published also all reported the synthesis of this compound, but the raw materials used all contain expensive cyclopropyl acetonitrile, which is also not easy to scale production

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