| 摘要 |
<p>A process for the preparation of (1S,2R)-1,2-epoxy-1,2,3,4-tetrahydronaphthalene having formula (I), which comprises the steps of (a) hydrogenating the compound of formula (II) to form c^_i^_s^_-(1R,2S)-1,2-dihydroxy-1,2,3,4-tetrahydronaphthalene having formula (V); (b) reacting the dihydroxy compound of formula (V) with a sulphonyl halide of formula R1SO2Z wherein R1 is methyl, ethyl, trifluoromethyl, phenyl or p^_-tolyl, and Z is fluorine, chlorine, bromine or iodine to give a bis-sulphonyl ester of formula (X); and (c) treating the bis-sulphonyl ester (X) with an alkali metal carbonate or alkali metal hydroxyde to give the compound of formula (I). A process for preparing the enantiomeric (1R,2S)-1,2-epoxy-1,2,3,4-tetrahydronaphthalene is also claimed as are novel intermediates formed in the processes. The compounds are useful as intermediates in the preparation of biologically active compounds such as pharmaceuticals.</p> |
