Preparation of atorvastatin

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

Reexamination Certificate

active

10800741

ABSTRACT:
A process for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester comprising:(a) reduction of 5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-oxo-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester;(b) hydrolysis of (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester using an alkali base in a solvent to form the acid;(c) alkylation of the acid forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester.

REFERENCES:
patent: 5273995 (1993-12-01), Roth
Brooks, D.W., et al. “C-Acylation under Virtually Neutral Conditions”,Angew. Chem. Int. Ed. Engl., (1979) 18, No. 1, pp. 72-74.
Brower, P.L., et al., “The Synthesis of (4R-cis)-1,1-Dimethylethyl 6-cyanomethyl-2,2-dimethyl-1,3-dioxane-4-acetate, a Key Intermediate for the Preparation of Cl-981, a Highly Potent, Tissue Selective Inhibitor of HMG-CoA Reductase”,Tetrahedron Letters, (1992) vol. 33, No. 17, pp. 2279-2282.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Preparation of atorvastatin does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Preparation of atorvastatin, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Preparation of atorvastatin will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-3735309

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.