Intramolecular arbuzov process for the preparation of intermediates useful in the preparation of phosphorus containing HMG-COA reductase inhibitors
US5274155A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 7, 1992 |
| Grant date | Dec 28, 1993 |
| Priority date | — |
| Expiry date | Dec 7, 2012 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F9/6506
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A process for the preparation of compounds of formula ##STR1## and pharmaceutically acceptable salts thereof; wherein X is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C-- or --CH.sub.2 O-- (where O is linked to Z); Z is a hydrophobic anchor R.sub.1 is hydrogen, alkyl, cycloalkyl or aryl; comprising the steps of: PA0 (A) reacting a compound of formula ##STR2## with a compound of formula ##STR3## or a compound of formula ##STR4## in the presence of an amine base or an alkali metal hydride in an organic solvent to form a compound having the formula ##STR5## (B) heating the compound of formula IX at a temperature of from about 100.degree. C. to about 200.degree. C., to form a compound of formula ##STR6## and (C) quenching the compounds of formula VIII with an acid provides the compounds of formula I.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.