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US 9,850,215 B2Granted
5-fluoro-4-imino-3-(alkyl/substituted alkyl)-1-(arylsulfonyl)-3,4-dihydropyrimidin-2(1 H)-one and processes for their preparation
AssigneeAdama Makhteshim Ltd.
InventorsNakyen Choy, Ronald Ross, Jr.
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Abstract
Provided herein are 5-fluoro-4-imino-3-(alkyl/substituted alkyl)-1-(arylsulfonyl)-3,4-dihydropyrimidin-2(1H)-one and processes for their preparation which may include the use of an alkali carbonate and an alkylating agent
Claims13
A method of making compounds of Formula III, including the steps of:
- contacting a compound of Formula II with an alkali carbonate and an alkylating agent,
- and
- forming a compound of Formula III:
- wherein R1 is selected from the group consisting of:
- and
- and
- R2 is selected from the group consisting of:
- wherein the molar ratio of the compound of Formula II to the alkali carbonate is from 3:1 to 1:1.
5 more elements
A method of preparing a compound of Formula II, including the steps or:
- contacting a compound of Formula I:
- with bis-N,O-trimethylsilylacetamide;
- and
- forming a compound of Formula II:
- wherein R1 is selected from the group consisting of:
- and
- wherein the molar ratio of compound I to bis-N,O-trimethylsilylacetamide is 1:1.1 and the contacting step is carried out at 22° C. to 70° C.
4 more elements
Dependencies are inferred from the claim text.