# US 7,608,731 B2 · Phenylacetic acid compounds

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- Number: US 7,608,731 B2
- Document ID: US7608731B2
- Status: Granted
- Kind: B2
- Application number: 11/977,262
- Filed: 2007-10-23
- Published: 2008-05-08
- Granted: 2009-10-27
- Earliest claimed: 2004-04-15
- Assignees: Roche Palo Alto LLC
- Inventors: Denis John Kertesz; Michael Martin; Wylie Solang Palmer
- Web page: https://patentgrep.com/patent/US7608731B2

## CPC

- C07D 209/08: with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
- A61P 31/18: for HIV
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 233/65: having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C 235/46: having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C 253/30: by reactions not involving the formation of cyano groups
- C07C 255/54: containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
- C07D 209/32: Oxygen atoms
- C07D 213/65: attached in position 3 or 5
- C07D 237/14: Oxygen atoms
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

The present invention provides a process for the preparation 6-[3-(hetero)aryloxy-2-fluoro-benzyl]-2H-pyridazin-3-one compounds 1 where R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R6 is NO2, NH2, alkyl, halogen, or a function group readily derived therefrom and R4c is hydrogen or alkyl. There also is provided a process for the preparation of phenylacetic acid compounds 2, wherein R2 and R6 are as defined previously and R5a is hydrogen or alkyl, which are useful for the preparation of pyridazinone compounds.

## Claims

### Claim 1

A compound according to formula Va wherein:
R2 is an aryl radical and said aryl radical is optionally substituted with zero to three substituents independently selected from the group consisting of C1-6 alkyl, C1-6 alkenyl, C1-6 haloalkyl, C3-8 cycloalkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 sulfonyl, C1-6 haloalkoxy, C1-6 haloalkylthio, hydroxyl, halogen, amino, C1-6 alkylamino, C1-6 dialkylamino, C1-6 N,N-dialkylcarbamoyl, nitro and cyano;
R4a is in each occurrence is independently hydrogen, C1-6 alkyl or benzyl;
R5 is H or CO2R5a: and
R5a is independently in each occurrence a straight or branched C1-6 alkyl.