- Synthesis method of efinaconazole intermediate
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Belonging to the field of biomedical industry, the invention discloses a synthesis method of an efinaconazole intermediate VI. The method includes: taking benzyl as a hydroxyl protecting group to generate a new compound II, then carrying out Grignard reaction, epoxidation reaction and epoxy ring-opening reaction on the compound II, and finally carrying out deprotection reaction to obtain the efinaconazole intermediate VI. The preparation method provided by the invention adopts benzyl as the hydroxyl protecting group, improves the problem of easy ring opening of tetrahydropyrane protecting group under an acidic condition in an original method, and at the same time has the advantages of good product purity and high yield.
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- Process for the preparation of 2-hydroxyalkyl halophenones
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2-Benzyloxyalkyl halophenones of the formula (3): wherein X1and X2are each independently H, Cl or F, provided that at least one of X1and X2is Cl or F; one of R3and R4is H and the other is optionally substituted benzyloxy; and R5is an unsubstituted alkyl, preferably a C1-6alkyl group. The compounds are useful as intermediates for preparing 2-hydroxyalkyl halophenones.
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