Process for the preparation of fluoxastrobin and intermediates thereof
AssigneeUpl Ltd
InventorsDigishkumar Manubhai Panchal, Pareshkumar Kalyanji Tandel
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Abstract
The invention provides an improved process for the preparation of fluoxastrobin and intermediates thereof. The present invention provides a process for the preparation of fluoaxastrobin, 4,6-dichloro-5-fluoro-pyrimidine and diethyl 2-chloromalonate that are substantially free of unwanted impurities.
Claims21
A process for the preparation of fluoxastrobin via the intermediate of formula (1), or via the intermediate of formula (5) prepared via the intermediate of formula (1):
- wherein the intermediate of formula (1) is prepared by chlorinating a compound of formula (2):
- with chlorine, wherein the concentration of reactive chlorine in the reaction medium during the reaction is between 0.01 to 5 mol %/minute and wherein R═C1-C4 alkyl, wherein the reaction is carried out at a temperature in a range of 5 to 20° C. for a period of 1 to 6 hours.
A process for the preparation of a 4,6-dichloro-5-fluoro-pyrimidine of formula (5) comprising:
- via the intermediate of formula (1)
- wherein the intermediate of formula (1) is obtained by chlorinating a compound of formula (2)
- with chlorine, wherein the concentration of reactive chlorine in the reaction medium during the reaction is between 0.01 to 5 mol %/minute.
A process for the preparation of a compound of formula (1) comprising:
- chlorinating a compound of formula (2)
- with chlorine, wherein the concentration of reactive chlorine is in the range of 0.01 to 5 mol %/minute and wherein R═C1-C4 alkyl.
A process for preparation of a 4,6-dichloro-5-fluoro-pyrimidine of formula (5) comprising:
- (i) chlorinating a compound of formula (2)
- with chlorine, wherein the concentration of reactive chlorine is between 0.01 to 5 mol %/minute to provide a compound of formula (1) substantially free of dihalo malonate impurity of formula (10)
- (ii) treating the compound of formula (1) with a fluorinating agent to get a compound of formula (3)
- wherein R═C1-C4 alkyl;
- (iii) reacting the compound of formula (3) with formamide or its derivatives to provide a compound of formula (4);
- and
- (iv) treating the compound of formula (4) with a chlorinating agent to provide the 4,6-dichloro-5-fluoro-pyrimidine of formula (5)
Dependencies are inferred from the claim text.