Process for the preparation of cyclopropylacetylene and its derivatives

摘要

According to the present invention, a process for the preparation of a cyclopropylacetylene derivative represented by the following formula (III): is provided, which comprises reacting a cyclopropylacrylic acid derivative represented by the following formula (I): with a halogenating agent to obtain a halogenocyclopropylpropionic acid derivative represented by the following formula (II): and reacting the halogenocyclopropylpropionic acid derivative with a base. In the above formulae, R<1>,R<2>,R<3>,R<4> and R<5> represent a hydrogen atom or an eventually substituted alkyl group, R<6> and R<8> represent a hydrogen atom, an eventually subtituted alkyl group or an eventually protected carboxyl group, R<7> represents a hydrogen atom or a carboxyl protecting group, and X and Y represent a halogen atom.