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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