| 摘要 |
<p>The present invention refers to an improved process of producing Amorolfine base, which is a compound of formula (I):
said process comprising the steps of:
(i) contacting a compound of formula (II):
with a Friedel-Crafts catalyst; and
(ii) adding one equivalent of 2-halogeno-2-methylbutane,
characterised in that the reaction mixture obtained in step (i) is cooled to a temperature between -40 to -60 °C prior to step (ii) and the Friedel-Craft catalyst is chosen among the group consisting of boron trifluoride complex, titanium chloride complex, zinc chloride, gallium chloride, antimony pentafluoride, molybdenum pentachloride, indium chloride, antimony pentachloride, lanthanide bromide, scandium(III)triflate, lanthanide (III) triflate, yterbium (III) triflate and silica gel associated with ferric chloride.</p> |
