Patent · US Active

Preparation of alkyl 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid ester

US8871947B2 · kind B2 · utility

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15References
17Claims
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Key dates

Filing dateDec 31, 2013
Grant dateOct 28, 2014
Priority date
Expiry dateDec 31, 2033

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07C69/738
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The present disclosure provides a novel and economically advantageous process for preparation of compounds of Formula I, such as alkyl 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid ester. The process includes acidification of the sodium enolate of alkyl difluoroacetoacetate by carbonic acid generated in situ by reacting carbon dioxide with water. The disclosure also includes promoting the ring closure reaction in which alkyl 2-alkomethylene-4,4-difluoro-3-oxobutyrate is reacted with methylhydrazine in two phase system with a weak base such as Na2CO3 or K2CO3.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.