EP 1480943 A2 20041201 - SYNTHESIS OF 3,5-DIHYDROXY-7-PYRROL-1-YL HEPTANOIC ACIDS
Title (en)
SYNTHESIS OF 3,5-DIHYDROXY-7-PYRROL-1-YL HEPTANOIC ACIDS
Title (de)
SYNTHESE VON 3,5-DIHYDROXY-7-PYRROL-1-YL-HEPTANSÄUREN
Title (fr)
SYNTHESE D'ACIDES 3,5-DIHYDROXY-7-PYRROL-1-YLE HEPTANOIQUES
Publication
Application
Priority
- US 0337026 W 20031117
- US 42634202 P 20021115
- US 46611403 P 20030429
- US 48044003 P 20030623
- US 48338103 P 20030627
Abstract (en)
[origin: WO2004046105A2] Atorvastatin and related 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acids can be made by oxidation of a 3,5-dihydroxy-7-pyrrol-1-yl heptanol precursor from novel but readily accessible starting materials. Silylether-protected 7-amino-3,5-dihydroxy heptanoic acid esters undergo Paal Knorr reaction with 1,4-diketones to give valuable silylether-diprotected 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acid ester intermediates for preparing atorvastatin. The Paal Knorr reaction of ketal-proctected 7-amino-3R, 5R-dihydroxy heptanoic acid esters with 4-fluoro-alpha-(2-methyl-1-oxopropyl-gamma-oxo-N,beta-diphenylbenzenebutanamide occurs in high yield with few side products when it is conducted in a low boiling point ether.
IPC 1-7
IPC 8 full level
C07D 319/06 (2006.01); C07D 405/06 (2006.01); C07F 7/18 (2006.01)
CPC (source: EP)
C07C 215/10 (2013.01); C07D 207/34 (2013.01); C07D 319/06 (2013.01); C07D 405/06 (2013.01); C07F 7/1892 (2013.01)
Citation (search report)
See references of WO 2004046105A2
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LI LU MC NL PT RO SE SI SK TR
DOCDB simple family (publication)
WO 2004046105 A2 20040603; WO 2004046105 A3 20041007; AU 2003295684 A1 20040615; AU 2003295684 A8 20040615; EP 1480943 A2 20041201
DOCDB simple family (application)
US 0337026 W 20031117; AU 2003295684 A 20031117; EP 03786885 A 20031117