| 摘要 |
<p>A process for the preparation of a cyclopropylacetylene derivative of the formula (V): <CHEM> comprises the steps of reacting a propynol derivative of the formula (I): <CHEM> with a propane derivative of the formula (VI): <CHEM> in the presence of a base in an amount of 2 or more equivalents relative to the propynol derivative to give a cyclopropane derivative of the formula (III): <CHEM> deprotecting the protecting group for the hydroxyl group of the cyclopropane derivative to give a cyclopropylpropynol derivative of the formula (IV): <CHEM> and subjecting the cyclopropylpropynol derivative to retro-ethynylation. In the above formula R<1>, R<2>, R<3>, R<4> and R<5> represent a hydrogen atom, or an alkyl, alkenyl, aryl or aralkyl each of which may have a substituent, R<6> and R<7> represent a hydrogen atom, or an alkyl, alkenyl, aryl or aralkyl each of which may have a substituent, or R<6> and R<7> may together form a ring, R<8> represents a protecting group for a hydroxyl group and X and Y represent a leaving group.</p> |
