43024-15-3

Usage

Uses

Used in Chemical Research:
3-Amino-4-ethylpyrazole is used as a chemical intermediate for conducting research in the field of organic chemistry. Its unique structure allows for further functionalization and modification, making it a valuable building block for the synthesis of more complex molecules.
Used in Pharmaceutical Industry:
3-Amino-4-ethylpyrazole is utilized as a key intermediate in the development of pharmaceutical compounds. Its presence in the molecular structure can contribute to the desired biological activity of the final drug, making it an essential component in the synthesis of various therapeutic agents.

InChI:InChI=1/C5H9N3/c1-2-4-3-7-8-5(4)6/h3H,2H2,1H3,(H3,6,7,8)

Upstream product

• 109-74-0 propyl cyanide 
• 107-31-3 Methyl formate 
• 43024-14-2 α-formyl-n-butyronitrile 
• 109-94-4 formic acid ethyl ester 
• 1010800-27-7 3-amino-4-ethylpyrazole oxalate 

Downstream Products

• 2020052-55-3 (S)-N-(3-(3-ethyl-5-(2-(2-hydroxyethyl)piperidin-1-yl)pyrazolo[1,5-a]pyrimidin-7-ylamino)phenyl)acrylamide 
• 2020052-55-3 (R)-N-(3-(3-ethyl-5-(2-(2-hydroxyethyl)piperidin-1-yl)pyrazolo[1,5-a]pyrimidin-7-ylamino)phenyl)acrylamide 

Relevant academic research and scientific papers

CDK inhibitor based on organic arsine as well as preparation method and application of CDK inhibitor

The invention provides a CDK inhibitor based on organic arsine as well as a preparation method and application of the CDK inhibitor. Specifically, the invention providese compounds of Formula I, or stereoisomers or tautomers thereof, or pharmaceutically acceptable salts, hydrates or solvates thereof; and the invention also discloses a preparation method and application thereof. Definitions of allgroups in the formula are shown in the specification.

Structure-Based Design of Selective Noncovalent CDK12 Inhibitors

Cyclin-dependent kinase (CDK) 12 knockdown via siRNA decreases the transcription of DNA-damage-response genes and sensitizes BRCA wild-type cells to poly(ADP-ribose) polymerase (PARP) inhibition. To recapitulate this effect with a small molecule, we sought a potent, selective CDK12 inhibitor. Crystal structures and modeling informed hybridization between dinaciclib and SR-3029, resulting in lead compound 5 [(S)-2-(1-(6-(((6,7-difluoro-1H-benzo[d]imidazol-2-yl)methyl)amino)-9-ethyl-9H-purin-2-yl)piperidin-2-yl)ethan-1-ol]. Further structure-guided optimization delivered a series of selective CDK12 inhibitors, including compound 7 [(S)-2-(1-(6-(((6,7-difluoro-1H-benzo[d]imidazol-2-yl)methyl)amino)-9-isopropyl-9H-purin-2-yl)piperidin-2-yl)ethan-1-ol]. Profiling of this compound across CDK9, 7, 2, and 1 at high ATP concentration, single-point kinase panel screening against 352 targets at 0.1 μm, and proteomics via kinase affinity matrix technology demonstrated the selectivity. This series of compounds inhibits phosphorylation of Ser2 on the C-terminal repeat domain of RNA polymerase II, consistent with CDK12 inhibition. These selective compounds were also acutely toxic to OV90 as well as THP1 cells.

PYRAZOLO[1,5-A][1,3,5]TRIAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AS CDK INHIBITORS

The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L1, L2, R1,R2, R3, R4, R6, m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.

Synthesis of3H-, 13C3-, and 14C-labeled Sch 727965

The preparation of [3H]Sch 727965 from unlabeled compound and tritiated water was base catalyzed. Diethyl [13C3]malonate was used to prepare [13C3]Sch 727965 in five steps in 21.8% overall yield. In a similar manner, [14C]Sch 727965 was prepared in five steps from diethyl [2-14C]malonate in 11.1% radiochemical yield. Copyright

Synthesis of 3-amino-4-substituted pyrazole derivatives

This application discloses a novel process to synthesize 3-amino-4-substituted pyrazole derivatives, which may be used, for example, as intermediates to prepare compounds having, for example, pharmaceutical utility.

Pyrazolotriazines as kinase inhibitors

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]triazine compounds as inhibitors of kinases such as, for example, cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing

PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Studies on nonpeptide angiotensin II receptor antagonists. I. Synthesis and biological evaluation of pyrazolo [1,5-b][1,2,4]triazole derivatives with alkyl substituents

Alkyl-substituted pyrazolo[1,5-b][1,2,4]triazole derivatives were synthesized and evaluated for activity as angiotensin II receptor antagonists. Molecules with the (methylbiphenylyl)tetrazole moiety at N-5 were the preferred compounds. Ethyl substitutions

Pyrazolotriazole derivatives

This invention relates to a pyrazolotriazole derivative represented by the general formula: STR1 wherein each symbol means as follows; R1, R3 and R4 : one of them represents hydrogen, tetrazolylated biphenylmethyl or lower