| 摘要 |
The present invention relates to a new process for the preparation of bicyclic lactones having the general formula (I) wherein Ar is an aryl radical, preferably phenyl. The new process of the invention in two steps comprises reacting an aryl-acetate of alkyl with halomethyl epoxy in an appropriate solvant in the presence of an alkali metal alcoolate, and proceeding directly to the acid hydrolysis of the resulting product. By implementing the process of the invention, the use of NaNH2 is avoided in the first step, and the second step of hydrolysing the nitril function by means of NaOH 10N is suppressed, but was necessary for the prior process before the acid hydrolysis by HC1 2N. The bicyclic lactones obtained by the process of the invention are particularly useful for the preparation of milnacipran (Ar = phenyl).
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