| 摘要 |
<p>Cyclohexane diol derivatives of formula (I) are prepd. from 1L-1,2,5/3 cyclohexane tetrol (II) by treatment with an aryl sulphonyl chloride (III) at -5 to +5 degrees C. (where R = aryl sulphonyl). (I) are intermediates for the prepn. of synthetic aminoglycoside antibiotics as described in BE 825456. The method is much simpler to carry out on an industrial scale than the known method of making (I), and gives better yields (65-70% overall, as compared with 34%). The pref. cpds. (I) are those where R = tosyl or p-bromo benzene sulphonyl. The reaction is pref. effected in pyridine at 0 degrees C. In an example 2.93g (II) in 10 ml pyridine was treated at 0 degrees C with 9.5g (III, R = tosyl) to give 73% yield of (I, R = tosyl) m.pt.</p> |
