119083-00-0

Usage

Chemical Properties

White solid

InChI:InChI=1/C6H5F3N2O2/c1-11-4(6(7,8)9)3(2-10-11)5(12)13/h2H,1H3,(H,12,13)

Upstream product

• 231285-86-2 ethyl 5-(trifluoromethyl)-1-methyl-1H-pyrazole-4-carboxylate 
• 111493-74-4 ethyl 3-(trifluoromethyl)-1-methyl-1H-pyrazole-4-carboxylate 
• 124-38-9 carbon dioxide 
• 153085-15-5 1-methyl-5-(trifluoromethyl)-1H-pyrazole 

Relevant academic research and scientific papers

Preparation method for polyfluoromethylpyrazole compound, and intermediate of compound and preparation method thereof

The invention discloses a preparation method for a polyfluoromethylpyrazole compound, and an intermediate of the compound and a preparation method thereof. The invention provides a preparation method for a compound 1 as defined in the specification. The preparation method comprises a step of subjecting a compound 2 as defined in the specification and methylhydrazine to a ring-closure reaction in an organic solvent so as to obtain the compound 1, wherein R is a C1-4 alkyl group, R is a methyl or ethyl group and x is 2 or 3. The preparation method provided by the invention uses cheap and easily available raw materials and is mild in reaction conditions, safe to operate, environment friendly, low in production cost, high in reaction conversion rate, low in the content of isomer in by-products, high in reaction yield and product purity and suitable for industrial production.

COMPOUNDS USEFUL AS CSF1 MODULATORS

This invention relates to novel compounds and to pharmaceutical compositions comprising the novel compounds. More specifically, the invention relates to compounds useful as Colony Stimulating Factor 1 Receptor (cFMS) modulators (e.g. cFMS inhibitors). This invention also relates to processes for preparing the compounds, uses of the compounds in treatment and methods of treatment employing the compounds. Specifically, the invention relates to the use of the compounds for the treatment of cancer and autoimmune diseases.

Method of manufacturing pyrazolecarboxylic compd.

PROBLEM TO BE SOLVED: To provide 1,3-disubstituted pyrazole-4-carboxylic acid obtained by reducing the content of isomers from 1,3-disubstituted pyrazole-4-carboxylic acid containing 1,5-disubstituted pyrazole-4-carboxylic acid (the isomer). SOLUTION: The production method of 1,3-disubstituted pyrazole-4-carboxylic acid comprises: preparing an aqueous solution including 1,3-disubstituted pyrazole-4-carboxylate, 1,5-disubstituted pyrazole-4-carboxylate and an organic solvent; and making the pH of this aqueous solution to the pH range where the 1,3-disubstituted pyrazole-4-carboxylic acid precipitates. COPYRIGHT: (C)2013,JPOandINPIT

Switchable reactivity: The site-selective functionalization of trifluoromethyl-substituted pyrazoles

Modern organometallic methods enable the regioflexible conversion of simple heterocyclic starting materials into families of isomers and congeners. Depending on the choice of the reagent, 1-methyl-5-(trifluoromethyl)pyrazole (1) undergoes deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. Similarly, 1-phenyl-5-(trifluoromethyl)pyrazole (5) and 3-methyl-l-phenyl-5-(trifluoromethyl)pyrazole (8) are selectively attacked by lithium diisopropylamide at the heterocyclic 4-position and by butyllithium concomitantly at the 4-position and the ortho position of the phenyl ring. In contrast, metalation of 1-methyl-3-(trifluoromethyl)pyrazole (2) occurs only at the 5-position, whatever the organometallic or metal amide base. Further sites become accessible to functionalization if bromine is introduced into the heterocyclic or aromatic ring. This has been demonstrated with 4-bromo-1-methyl-5-(trifluoromethyl)pyrazole (3), 4-bromo-l-methyl-3-(trifluoromethyl)pyrazole (4), 4-bromo-1-methyl-5-(trifluoromethyl)pyrazole (7) and 1-(2-bromophenyl)-5-(trifluoromethyl)pyrazole (6). Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002.