15754-60-6

Usage

Uses

Used in Pharmaceutical Industry:
1-tert-Butyl-1H-pyrazole is used as a pharmaceutical intermediate for the development of new drugs. Its unique molecular structure and potential biological activities make it a valuable compound for designing and synthesizing novel therapeutic agents.
Used in Organic Synthesis:
1-tert-Butyl-1H-pyrazole serves as a building block in organic synthesis, contributing to the creation of various organic compounds. Its tert-butyl group provides steric hindrance, which can enhance the compound's stability and reactivity in chemical reactions, making it a useful component in the synthesis of complex organic molecules.
Used in Drug Development:
Due to its potential biological activities and unique molecular structure, 1-tert-Butyl-1H-pyrazole is utilized in drug development for the exploration of its therapeutic potential. Further investigation into its properties may lead to the discovery of new drugs with improved efficacy and safety profiles.

Upstream product

• 288-13-1 NH-pyrazole 
• 507-20-0 tertiary butyl chloride 
• 102-52-3 malonaldehydebis(dimethylacetal) 
• 7400-27-3 tertbutylhydrazine hydrochloride 

Downstream Products

• 288-13-1 NH-pyrazole 
• 115-11-7 isobutene 
• 97421-12-0 1-tert-butyl-4-nitropyrazole 
• 70951-85-8 4-bromo-1-(1,1-dimethylethyl)-1H-pyrazole 
• 1256359-15-5 1-(1,1-dimethylethyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole 
• 1354705-41-1 1-(tert-butyl)-4-iodo-1H-pyrazole 

Relevant academic research and scientific papers

PYRAZOLYL-SUBSTITUTED HETEROARYLS AND THEIR USE AS MEDICAMENTS

The invention relates to new substituted heteroaryls of formula 1 or of formula 1' wherein A is either N or CH, wherein R2 is selected from the group consisting of -C1-3-alkyl, -C1-3-haloalkyl, F, Br, CI, wherein Y is selected from -O- or -CH2-, and wherein R3 is defined as in claim 1, and the pharmaceutically acceptable salts thereof, and the use of these aforementioned compounds for the treatment of diseases such as asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.

5-AZAINDAZOLE COMPOUNDS AND METHODS OF USE

5-Azaindazole compounds of Formula (I), including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

7-(lH-PYRAZOL-4-YL)-1,6-NAPHTHYRIDINE COMPOUNDS AS SYK INHIBITORS

The present invention relates to a compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast and/or basophil cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, chronic spontaneous urticaria and autoimmune conditions.

7-(1H-PYRAZOL-4-YL)-1,6-NAPHTHYRIDINE COMPOUNDS AS SYK INHIBITORS

A compound of formula (I) or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast and/or basophil cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, chronic spontaneous urticaria and autoimmune conditions.

KINASE INHIBITORS USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES

The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

Process for preparing N-substituted pyrazoles

A process for the preparation of an N-alkyl- or N-phenylalkyl-substituted pyrazole I by reacting the corresponding N-unsubstituted pyrazole II with an alcohol III of the formula R1 --OH where R1 is the same alkyl or phenylalkyl group to be added to the unsubstituted nitrogen group --NH-- of the pyrazole reactant. Both of the reactants, i.e. the pyrazole II and alcohol III compounds, are catalytically reacted in the liquid phase in a molar ratio of from 0.001:1 to 1:1, at temperatures of 50°-400° C. and under a subatmosheric pressure of from 0.8 bar up to a superatmospheric pressure of 250 bar. The catalyst required for this liquid phase reaction is selected as being at least one or more non-heterogeneous acid catalysts, their alkyl esters or their acid anhydrides.

Influence of N-substitution in the FVT of pyrazoles

Flash vacuum thermolysis of 1-ethyl (3), 3,5-dimethyl-1-ethyl (4), 1-n-buthyl (5), 1-tert-butyl (6), 3,5-dimethyl-1-phenyl (7) and 1-phenyl-pyrazole (8) was studied.In the N-alkyl derivatives, pyrazole elimination and olefin formation was found.In contrast, phenylderivatives afforded isomerization and nitrogen extrusion.Kinetic parameters for compound 4 are described and a general mechanism including the N-H derivatives is discussed.