540752-87-2

Usage

Uses

Used in Pharmaceutical Industry:
3-[4-(N-Boc)piperazin-1-yl]phenylboronic acid pinacol ester is used as a key building block for the synthesis of various pharmaceutical compounds. Its presence in the molecule allows for the creation of diverse drug candidates with potential therapeutic applications.
Used in Organic Synthesis:
In the field of organic synthesis, 3-[4-(N-Boc)piperazin-1-yl]phenylboronic acid pinacol ester serves as a valuable reagent for Suzuki-Miyaura coupling reactions. These reactions are essential for the formation of biaryl compounds, which are prevalent in numerous pharmaceuticals, agrochemicals, and materials science applications.
Used in Enhancing Stability:
The pinacol ester moiety in 3-[4-(N-Boc)piperazin-1-yl]phenylboronic acid pinacol ester is used to enhance the stability of the boronic acid group. This stability allows for easier handling and storage of the compound, making it more accessible for use in various chemical processes and applications.
Overall, 3-[4-(N-Boc)piperazin-1-yl]phenylboronic acid pinacol ester is a crucial chemical intermediate with applications spanning across the pharmaceutical industry, organic synthesis, and as a stabilizer for boronic acid groups. Its versatility and importance in the synthesis of biologically active compounds make it a valuable asset in the field of chemistry.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 31197-30-5 1-(3-bromophenyl)piperazine 
• 108-36-1 1,3-dibromobenzene 
• 73183-34-3 bis(pinacol)diborane 
• 327030-39-7 1,1-dimethylethyl 4-(3-bromophenyl)piperazine-1-carboxylate 
• 123-91-1 1,4-dioxane 
• 571202-87-4 3-bromophenyl triisopropylsilyl ether 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 862261-23-2 4-(3-triisopropylsilanyloxy-phenyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 198627-86-0 1,1-dimethylethyl 4-(3-hydroxyphenyl)-1-piperazinecarboxylate 
• 540752-86-1 4-(3-trifluoromethanesulfonyloxy-phenyl)-piperazine-1-carboxylic acid tert-butyl ester 

Downstream Products

• 540752-88-3 4-[3-(2-amino-6-chloro-pyrimidin-4-yl)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 540752-08-7 2-furan-2-yl-7-(3-piperazin-1-yl-phenyl)-[1,2,4]triazolo[1,5-c]pyrimidin-5-ylamine 
• 540751-83-5 4-[3-(5-amino-2-furan-2-yl-[1,2,4]triazolo[1,5-c]pyrimidin-7-yl)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 1138473-18-3 {5-methyl-4-[5-(3-piperazin-1-yl-phenyl)-thiophen-2-yl]-pyrimidin-2-yl}-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine 
• 1370453-96-5 N-[6-(3-piperazin-1-ylphenyl)pyridin-2-yl]-4-(trifluoromethyl)pyridin-2-amine 
• 1370454-38-8 N-[6-(3-piperazin-1-ylphenyl)pyridin-2-yl]pyrazin-2-amine 
• 1370454-40-2 tert-butyl 4-{3-[6-(pyrazin-2-ylamino)pyridin-2-yl]phenyl}piperazine-1-carboxylate 
• 1370453-99-8 tert-butyl 4-[3-(6-aminopyridin-2-yl)phenyl]piperazine-1-carboxylate 
• 1312595-13-3 3-chloro-N-[6-methyl-3-[3-(1-piperazinyl)phenyl]-2-(1H-pyrazol-4-yl)thieno[2,3-b]pyridin-4-yl]benzenesulfonamide 
• 1312594-16-3 1,1-dimethylethyl 4-[3-(4-amino-2,6-dimethylthieno[2,3-b]pyridin-3-yl)phenyl]-1-piperazinecarboxylate 

Relevant academic research and scientific papers

Receptor-interacting protein kinase 2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling inhibitors based on a 3,5-diphenyl-2-aminopyridine scaffold

Receptor-interacting protein kinase 2 (RIPK2) is a key mediator of nucleotide-binding oligomerization domain (NOD) cell signaling that has been implicated in various chronic inflammatory conditions. A new class of RIPK2 kinase/NOD signaling inhibitors bas

COMPOSITIONS FOR USE IN METHODS OF INHIBITING PROTEIN KINASES

Identified compounds demonstrate protein kinase inhibitory activity and inhibition of dependent cell signaling pathways, such as NOD2 cell signaling. More specifically, the compounds are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin- like kinase 2 (ALK2). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.

Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors

As demonstrated in preclinical animal models, the disruption of PI3Kδ expression or its activity leads to a decrease in inflammatory and immune responses. Therefore, inhibition of PI3Kδ may provide an alternative treatment for autoimmune diseases, such as RA, SLE, and respiratory ailments. Herein, we disclose the identification of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent, selective and orally bioavailable PI3Kδ inhibitors. The lead compound demonstrated efficacy in an in vivo mouse KLH model.

USP7 INHIBITOR COMPOUNDS AND METHODS OF USE

2-Aminopyridine compounds of Formula I are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for modulating USP7, and for treating cancer and immune disorders such as inflammation mediated by USP7. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

3-(PYRAZOLYL)-1H-PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS KINASE INHIBITORS

The present application relates to novel 3-(pyrazolyl)-lH-pyrrolo[2,3-b]pyridine derivatives of formula (I), as protein kinase inhibitors. The invention particularly relates to compounds of formula (I), preparation of compounds and pharmaceutical compositions thereof. The invention further relates to pharmaceutically acceptable salts and compositions comprising the said novel 3-(pyrazolyl)-lH-pyrrolo[2,3-b]pyridine derivatives and their use in the treatment of various disorders.

Highly potent aminopyridines as Syk kinase inhibitors

A novel class of potent Syk inhibitors has been developed from rational design. Highly potent aminopyridine derivatives bearing a 4-trifluoromethyl-2- pyridyl motif and represented by compound 13b IC50: 0.6 nM were identified. Substitution by a 2-pyrazinyl motif and SAR expansion in position 4 of the central core provided diverse potent non-cytotoxic Syk inhibitors showing nanomolar activity inhibiting human mast cell line LAD2 degranulation.

PYRIDINE AND ISOQUINOLINE DERIVATIVES AS SYK- AND JAK-KINASE INHIBITORS

The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by inhibition of Syk kinase and/or Janus kinases.

Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors

The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by inhibition of Syk kinase and/or Janus kinases.

PYRIDINE AND PYRAZINE DERIVATIVES - 083

The invention concerns pyridine and pyrazine derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of W, G1, G2, G3, G4, J, Ring A, n and R3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.

2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs as adenosine A2A antagonists: The successful reduction of hERG activity. Part 2

The structure-activity relationship (SAR) exploration using 2-(2-furanyl)-7-phenyl[1,2,4]triazolo-[1,5-c]pyrimidin-5-amine (1) as a template led to the identification of a novel class of potent and selective adenosine A2A receptor (AR) antagoni