| 摘要 |
A method for preparing t-butyl (R)-7-nitro-5-hydroxy-3-oxo-heptanoates is provided to produce chiral intermediates useful in a synthesis of atorvastatin in an economical and efficient manner. A method for preparing t-butyl (R)-7-nitro-5-hydroxy-3-oxo-heptanoates comprises the steps of: (i) subjecting (S)-3-hydroxy-butylactone represented by the formula 2 to a decyclization reaction in the presence of an iodine catalyst, acetic acid, ethanol, and hydrogen bromide, followed by reacting the resultant with nitromethane(CH3NO2) to prepare ethyl (R)-5-nitro-3-hydroxypentanoates represented by the formula 3; and (ii) subjecting the ethyl (R)-5-nitro-3-hydroxypentanoates represented by the formula 3 and t-butyl bromoacetate(BrCH2COOt-Bu) to a Grignard reaction using zinc or magnesium to prepare t-butyl (R)-7-nitro-5-hydroxy-3-oxo-heptanoates represented by the following formula 1.
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