US5159104A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Process to simvastatin ester
Assignee: Merck and Co Inc
•
Filing: 1991-05-01
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Granted: 1992-10-27
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Expires: 2011-05-01
Abstract
Abstract A process is disclosed, for the formation of simvastatin, which comprises the sequential acylation of a diol lactone to form a bis acylated intermediate followed by selective deacylation and lactone ring closure to form simvastatin.
Inventors
- 👤 Rebecca L. Dabora
- 👤 Gregory L. Tewalt
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 01:05
CPC Classifications
C; C07; C07D; C07D309/00; C07D309/16; C07D309/28; C07D309/30; A; A61; A61P; A61P3/00; A61P3/06; A61P9/00; A61P9/10; C07C; C07C69/00; C07C69/66; C07C69/73; C07C69/732
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
48 words
A process for the formation of a compound (IV) which comprises the treatment of a compound (III), wherein R is C 1-5 alkyl: ##STR2## with an alcohol R 1 OH, wherein R 1 is C 1-4 alkyl, and an acid to yield a compound of formula (IV): ##STR3##
Claim 2
Dependent Claim
48 words
A process for the formation of a compound (IV) which comprises the treatment of a compound (III), wherein R is C 1-5 alkyl: ##STR2## with an alcohol R 1 OH, wherein R 1 is C 1-4 alkyl, and an acid to yield a compound of formula (IV): ##STR3##
Claim 3
Dependent Claim
19 words
A process of claim 1 wherein the acid is selected from the group consisting of: hydrochloric, sulfuric, and acetic.
Claim 4
Dependent Claim
23 words
A process of claim 2 wherein the alcohol is selected from methanol, ethanol, n-propanol, isopropanol and t-butanol and the acid is hydrochloric acid.
Claim 5
Dependent Claim
51 words
A process further comprising the treatment of a diol lactone (I) ##STR4## with an acylating agent selected from (RCO) 2 O or RCOCl, wherein R is C 1-5 alkyl, to yield a compound (II): ##STR5## followed by treatment of compound (II) with 2,2-dimethylbutyryl chloride to yield a compound (III). ##STR6## ##STR7##
Claim 6
Dependent Claim
51 words
A process further comprising the treatment of a diol lactone (I) ##STR4## with an acylating agent selected from (RCO) 2 O or RCOCl, wherein R is C 1-5 alkyl, to yield a compound (II): ##STR5## followed by treatment of compound (II) with 2,2-dimethylbutyryl chloride to yield a compound (III). ##STR6## ##STR7##
References Cited (Backward Citations)
US4293496A
Cited
GB2073193A
Cited
US4444784A
Cited
US4582915A
Cited
US4584389A
Cited
JPS63303952A
Cited
US4820850A
Cited
US4866090A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1995-10-27 | 1996-04-27 | 1996-10-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-10-27 | 2000-04-27 | 2000-10-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-10-27 | 2004-04-27 | 2004-10-27 | $7700.00 | Window Closed / Lapsed |