# US 5,349,069 A · Process for the preparation of 4-phosphinyl-3-keto-carboxylate and 4-phosphonyl-3-keto-carboxylate intermediates useful in the preparation of phosphorus containing HMG-COA reductase inhibitors

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- Number: US 5,349,069 A
- Document ID: US5349069A
- Status: Granted
- Kind: A
- Application number: 08/171,284
- Filed: 1993-12-21
- Granted: 1994-09-20
- Earliest claimed: 1992-12-07
- Assignees: E. R. Squibb & Sons, Inc.
- Inventors: John K. Thottathil; Wen S. Li
- Web page: https://patentgrep.com/patent/US5349069A

## CPC

- C07F 9/5728: {condensed with carbocyclic rings or carbocyclic ring systems}
- C07F 9/301: {Acyclic saturated acids which can have further substituents on alkyl}
- C07F 9/3211: {Esters of acyclic saturated acids which can have further substituents on alkyl}
- C07F 9/3294: {Compounds containing the structure R2P(=X)-X-acyl, R2P(=X)-X-heteroatom, R2P(=X)-X-CN (X = O, S, Se)}
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)

## Abstract

A process for the preparation of compounds of formula ##STR1## or salt thereof where R.sub.1 is --X--Z and X is --C.tbd.C--, R.sub.2 and R.sub.2 ' are independently hydrogen, alkyl or trialkylsilyl; R.sub.3 is hydrogen or alkyl; and Z is a hydrophobic anchor; which includes reacting a compound of formula ##STR2## where R.sub.4 is alkyl, cycloalkyl or aryl; and R.sub.5 is trialkylsilyl or triarylsilyl with a compound of formula ##STR3## where Y is a halogen, to form a compound of formula ##STR4## and hydrolyzing the compound of formula IV to obtain the compounds of formula I. Compounds of formula I or salt thereof where R.sub.1 is --OR.sub.2 ' may be prepared by reacting a compound of formula III with a compound of formula P(OR.sub.2).sub.3. X

## Claims

### Claim 1

A compound of the formula ##STR20## where R.sub.1 is --X--Z or --OR.sub.2 ', where 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), and Z is ##STR21## R.sub.2 and R.sub.2 ' are independently hydrogen, alkyl or trialkylsilyl and R.sub.3 is hydrogen or alkyl.

### Claim 2

A compound of the formula ##STR22## where Z is ##STR23## R.sub.2 and R.sub.2 ' are independently hydrogen, alkyl or trialkylsilyl and R.sub.3 is hydrogen or alkyl.