Method for synthesizing pitavastatin t-butyl ester
OwnerHuan Huang, Kai Li +3inventors
InventorsHuan Huang, Kai Li, Qingyun Huang, Fuming Zhan, Qingguo Huang
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OwnerHuan Huang, Kai Li +3inventors
InventorsHuan Huang, Kai Li, Qingyun Huang, Fuming Zhan, Qingguo Huang
Estimating the term…
A method for synthesizing pitavastatin tert-butyl ester includes obtaining a substance B through reacting (4R-CIS)-6-chloromethyl-2,2-dimethyl-1,3-dioxolane-4-acetic acid tert-butyl ester with a substance A under the action of a first base catalyst, 5 oxidizing with an oxidizing agent to obtain a substance C, then reacting with 2-cyclopropyl-4-(4-fluorophenyl)-quinoline-3-formaldehyde under the action of a second base catalyst to obtain a substance D, and finally, carrying out an acid deprotection to obtain pitavastatin t-butyl ester. The reaction conditions of the present invention are mild and controllable, and the reaction conditions of the synthesis of the Julia olefination do 10 not require an ultra-low temperature reaction. The operation is convenient and simple, the stereoselectivity is good, the yield is high, and the synthesized pitavastatin t-butyl ester is a completely non-cis isomer, and its purity is high.
A method for synthesizing pitavastatin t-butyl ester, comprising the steps of:
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