A procedure for the prepn. of ezetimibe (I) and its new intermediate II is described. The procedure for the prepn. of I comprises: (i) Grignard reaction of amide III [R1, R2, independently, = C1-4-alkyl] with (4-fluorophenyl)magnesium bromide in an org. solvent; and, (ii) stereoselective redn. of the ketone function in II and successive deprotection of the hydroxyl group.
Allegrini, P., Naldini, D., Razzetti, G., Taddei, M. (2007)Procedure for the preparation of ezetimibe. . Brevetto No. IT 2007-MI2013.
Procedure for the preparation of ezetimibe
TADDEI, MAURIZIO
2007-01-01
Abstract
A procedure for the prepn. of ezetimibe (I) and its new intermediate II is described. The procedure for the prepn. of I comprises: (i) Grignard reaction of amide III [R1, R2, independently, = C1-4-alkyl] with (4-fluorophenyl)magnesium bromide in an org. solvent; and, (ii) stereoselective redn. of the ketone function in II and successive deprotection of the hydroxyl group.
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https://hdl.handle.net/11365/33945
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