US 9,000,221 B2 · Processes for the preparation of 4′-[3-[4-(6-Fluoro-1 ,2-benzisoxazol-3-yl)piperidino]propoxy]-3′-methoxyacetophenone and intermediates thereof

Abstract

The present invention relates to processes for the preparation of 4′-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino]propoxy]-3′-methoxyacetophenone and intermediates thereof. The present invention also provides a process for purifying 4′-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino]propoxy]-3′-methoxyacetophenone to obtain the purity greater than about 98.0 area % to about 99.0 area % as measured by HPLC, preferably greater than about 99.0 area % to about 99.5 area %, more preferably greater about 99.5 area % to about 99.9 area %. individual impurities lower than about 0.15 area %, preferably lower than about 0.1% and total impurities lower than about 0.5 area % by HPLC.

Claims4

Dependent claims

A process for preparing intermediate 4-(31-propoxy)-3-methoxyacetophenone compound of formula (II):

wherein X is a leaving group selected from halogen, methanesulphonate, benzenesulphonate, p-toluenesulphonate, 4-nitrobenzene sulphonate, 4-bromobenzene sulphonate and trifluoromethyl sulphonate, comprising:
reacting 1-[4-(31-propoxy)-3-methoxyphenyl]ethanol of formula (III):
where X is as defined above;
with an oxidizing agent, optionally in the presence of a solvent, wherein the oxidizing agent is selected from the group consisting of collin's reagent, pyridinium dichromate, pyridinium chlorochromate, pyridinium chlorochromate on alumina, DMSO-DCC, DMSO-acetic anhydride or mixtures thereof.

1 more element

Dependencies are inferred from the claim text.

Facts

Application

13/575,250Filed 18 Jul 2011

Priority

IN 2610/CHE/20107 Sep 2010

Published

US 2013/0190501 A125 Jul 2013

Granted

7 Apr 2015

Term ends

Not estimatedThe source records don’t support an estimate.

Classification8 codes

C07C 315/04
Preparation of sulfones; Preparation of sulfoxides: by reactions not involving the formation of sulfone or sulfoxide groups
C07C 45/004
Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds: by reaction with…
C07C 45/292
Of hydroxy groups: with chromium derivatives
C07C 303/30
Of esters of sulfonic acids: by reactions not involving the formation of esterified sulfo groups

Processes for the preparation of 4′-[3-[4-(6-Fluoro-1 ,2-benzisoxazol-3-yl)piperidino]propoxy]-3′-methoxyacetophenone and intermediates thereof

Life of this patent

Processes for the preparation of 4′-[3-[4-(6-Fluoro-1 ,2-benzisoxazol-3-yl)piperidino]propoxy]-3′-methoxyacetophenone and intermediates thereof

Life of this patent

Abstract

Claims4