The invention belongs to the technical field of pharmaceutical chemicals, and particularly discloses a bicyclo [2.1. 1]
hexane derivative as well as a preparation method and application thereof. The bicyclo [2.1. 1]
hexane derivative is a compound as shown in a formula (I) or a formula (II), a pharmaceutically acceptable salt, a stereoisomer or an
isotope label of the bicyclo [2.1. 1]
hexane derivative, wherein R1 is optionally selected from C1-C6
alkyl groups, bromomethyl
alkyl, benzyl
alkyl, ester groups, acylamino and acyl groups; r2 is optionally selected from
hydrogen, C1-C6 alkyl, benzyl alkyl,
aryl, heteroaryl, alkenyl,
halogen and
silicon; r3 is optionally selected from
hydrogen, C1-C6 alkyl, bromomethyl alkyl, benzyl alkyl, an ester group, an acylamino group, an
acyl group, an amido group, a
sulfenamide group,
halogen and a carboxyl group; and R4 is optionally selected from C1-C6 alkyl, benzyl alkyl,
aryl, heteroaryl and alkenyl. And the formula (II) can be obtained by carrying out half-
pinacol intramolecular rearrangement on the formula (I). Tests prove that the compounds in the formula (I) and the formula (II) can be used for treating
osteoarthritis diseases.