- Synthesis method of pyrazosulfuron-ethyl intermediate 4-ethoxycarbonyl-5-sulfamine-1-methylpyrazole
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The invention discloses a synthesis method of a pyrazosulfuron-ethyl intermediate 4-ethoxycarbonyl-5-sulfamine-1-methylpyrazole. The method comprises the following steps: (1) performing condensation reaction on 4-ethoxycarbonyl-5-hydroxyl-1-methylpyrazole and dimethylthiocarbamoyl chloride to obtain 4-ethoxycarbonyl-5-dimethylthio carbamoyl oxy-1-methylpyrazole; (2) performing transposition rearrangement reaction on the 4-ethoxycarbonyl-5-dimethylthio carbamoyl oxy-1-methylpyrazole to obtain 4-ethoxycarbonyl-5-dimethyl carbamoyl sulfenyl-1-methylpyrazole; (3) performing chlorosulfonation reaction on the 4-ethoxycarbonyl-5-dimethyl carbamoyl sulfenyl-1-methylpyrazole and chlorine to obtain 4-ethoxycarbonyl-5-sulfonyl chloride-1-methylpyrazole; (4) performing ammoniation reaction on the 4-ethoxycarbonyl-5-sulfonyl chloride-1-methylpyrazole and ammonium hydroxide to obtain the 4-ethoxycarbonyl-5-sulfamine-1-methylpyrazole. The method is less in environment pollution, particularly high in product purity, and high in total yield.
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Paragraph 0024; 0027
(2017/07/20)
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- Process for preparation of sulfonylurea derivatives and intermediates for the process and process for preparing the same
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The present invention relates to a novel process for preparing sulfonylurea derivatives of formula (I) in a high purity and a high yield characterized in that a sulfonylchloride of formula (V) is reacted with 2-amino-4,6-dimethoxypyrimidine of formula (VII) in the presence of a metal cyanate and an organic base catalyst or a compound of formula (VIII) is reacted with 2-amino-4,6-dimethoxypyrimidine of formula (VII): STR1 wherein R1 represents hydrogen, C1 -C4 alkyl or phenyl, R2 represents hydrogen, C1 -C4 alkyl, allyl or propargyl and R3 represents hydrogen, methyl, ethyl or phenyl, and to a process for preparing the sulfonylchloride compound of formula (V) above and the compound of formula (VIII) above, both of which are useful as an intermediate compound for preparing the sulfonylurea derivative of formula (I) and to a novel intermediate compound of formula (VIII) as defined above.
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- Process for the preparation of sulfonylurea derivatives and intermediates for this process
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The present invention relates to a novel process for preparing sulfonylurea derivatives of formula (I) in a high purity and a high yield characterized in that a sulfonylchloride of formula (V) is reacted with 2-amino-4,6-dimethoxypyrimidine of formula (VII) in the presence of a metal cyanate and an organic base catalyst or a compound of formula (VIII) is reacted with 2-amino-4,6-dimethoxypyrimidine of formula (VII): wherein R1 represents hydrogen, C1-C4 alkyl or phenyl, R2 represents hydrogen, C1-C4 alkyl, allyl or propargyl and R3 represents hydrogen, methyl, ethyl or phenyl, and to a process for preparing the sulfonylchloride compound of formula (V) above and the compound of formula (VIII) above, both of which are useful as an intermediate compound for preparing the sulfonylurea derivative of formula (I) and to a novel intermediate compound of formula (VIII) as defined above.
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