864754-18-7

Usage

Uses

Used in Pharmaceutical Industry:
1-(2-MORPHOLINOETHYL)-1H-PYRAZOLE-4-BORONIC ACID, PINACOL ESTER is used as a key intermediate in the synthesis of pharmaceutical compounds, leveraging its boronic acid functionality to form new bonds and create diverse medicinal agents.
Used in Agrochemical Industry:
In the agrochemical sector, 1-(2-MORPHOLINOETHYL)-1H-PYRAZOLE-4-BORONIC ACID, PINACOL ESTER is utilized as a reagent in the development of agrochemicals, potentially enhancing crop protection products through its ability to form complex molecular structures.
Used in Electronic Materials Development:
1-(2-MORPHOLINOETHYL)-1H-PYRAZOLE-4-BORONIC ACID, PINACOL ESTER is employed as a component in the creation of new materials for electronic devices, taking advantage of its structural properties to improve device performance.
Used in Optical Materials Development:
1-(2-MORPHOLINOETHYL)-1H-PYRAZOLE-4-BORONIC ACID, PINACOL ESTER is also used in the development of materials for optical devices, where its unique chemical structure may contribute to advancements in light manipulation and transmission technologies.
Used as a Building Block in Organic Synthesis:
1-(2-MORPHOLINOETHYL)-1H-PYRAZOLE-4-BORONIC ACID, PINACOL ESTER is used as a valuable building block for the synthesis of a variety of biologically active molecules, underpinning research and development efforts in creating new pharmaceuticals and other bioactive compounds.

InChI:InChI=1/C15H26BN3O3/c1-14(2)15(3,4)22-16(21-14)13-11-17-19(12-13)6-5-18-7-9-20-10-8-18/h11-12H,5-10H2,1-4H3

Upstream product

• 89583-07-3 N-(2-bromoethyl)morpholine 
• 269410-08-4 pyrazole-4-boronic acid pinacol ester 
• 3240-94-6 N-(2-chlorethyl)morpholine 
• 73183-34-3 bis(pinacol)diborane 
• 3647-69-6 4-(2-chloroethyl)morpholine hydrochride 
• 42802-94-8 4-(2-bromoethyl)morpholine hydrobromide 

Downstream Products

• 1032900-22-3 N₂-{2-isopropoxy-4-methyl-5-[1-(2-morpholin-4-yl-ethyl)-1H-pyrazol-4-yl]-phenyl}-5-methyl-N₄-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine 
• 1161737-38-7 (3-{5-[1-(2-morpholin-4-ylethyl)-1H-pyrazol-4-yl]pyrimidin-2-yl}-phenyl)methanol 
• 1403254-62-5 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-3-(methyl(tetrahydro-2H-pyran-4-yl)amino)-5-(1-(2-morpholinoethyl)-1H-pyrazol-4-yl)benzamide 
• 1403259-18-6 tert-butyl 4-((3-(((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)carbamoyl)-2-methyl-5-(1-(2-morpholinoethyl)-1H-pyrazol-4-yl)phenyl)(methyl)amino)piperidine-1-carboxylate 
• 1403254-90-9 3-(((1R,4R)-4-acetamidocyclohexyl)(methyl)amino)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-5-(1-(2-morpholinoethyl)-1H-pyrazol-4-yl)benzamide 
• 1403257-86-2 tert-butyl(((1S,4S)-4-(3-(((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)carbamoyl)-2-methyl-5-(1-(2-morpholinoethyl)-1H-pyrazol-4-yl)phenyl)(methyl)amino)cyclohexyl)carbamate 
• 1403257-94-2 tert-butyl ((1R,4R)-4-((3-(((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)carbamoyl)-2-methyl-5-(1-(2-morpholinoethyl)-1H-pyrazol-4-yl)phenyl)(methyl)amino)cyclohexyl)carbamate 

Relevant academic research and scientific papers

Design, synthesis and SAR study of 2-aminopyridine derivatives as potent and selective JAK2 inhibitors

The abnormal activation of JAK2 kinase is closely related to the occurrence and progression of myeloproliferative neoplasms (MPNs). At present, there is still an obvious unmet medical need for selective JAK2 inhibitors in clinic. In this paper, a class of 2-aminopyridine derivatives as potent and selective JAK2 inhibitors was obtained by combining drug design, synthesis and structure-activity relationship studies based on the previously identified lead Crizotinib. Among them, 21b exhibited high inhibitory activity against JAK2 with an IC50 of 9 9 nmol/L, moreover, it showed 276- and 184-fold selectivity over JAK1 and JAK3, respectively. Besides, 21b had a significant antiproliferative activity against HEL cells, and also inhibited the phosphorylation of JAK2 and its down-stream signaling pathway. These results indicated that 2-aminopyridine compound 21b had the potential to be developed as a selective JAK2 inhibitor for further study.

FGFR INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF

A compound having a structure of formula (I) and a preparation method therefor, and a use of the compound serving as an FGFR inhibitor for treating tumors, cancers, myeloproliferative diseases, bone or chondrocyte disorders, and hypophosphatemia.

N-(AZAARYL)CYCLOLACTAM-1-CARBOXAMIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF

An N-(azaaryl)cyclolactam-1-carboxamide derivative having a structure of formula (I), a preparation method therefor, and a use thereof are disclosed in the application. Each substituent are defined in the specification and claims. The series of compounds of the application can be widely applied in the preparation of drugs for treating cancer, tumor, autoimmune disease, metabolic disease or metastatic disease, particularly for treating ovarian cancer, pancreatic cancer, prostate cancer, breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic disease, neurodegenerative disease, primary tumor site metastasis or osseous metastasis cancer, and are expected to be developed into a new generation of CSF-1R inhibitor drugs.

Design, synthesis, and structure activity relationship (SAR) studies of novel imidazo[1,2-a] pyridine derivatives as Nek2 inhibitors

Never in mitosis (NIMA) related kinase 2 (Nek2) is involved in multiple cellular processes such as cell cycle checkpoint regulation, cell division, DNA damage response and cell apoptosis. Nek2 has been reported to be overexpressed in various tumors and correlated with poor prognosis. Herein, a series of imidazo[1,2-a] pyridines Nek2 inhibitors were designed, synthesized, and their biological activities were investigated. Besides, structure activity relationship analysis of these compounds were performed in the MGC-803 cell. The screening results are promising, and compound 28e shows good proliferation inhibitory activity with an IC50 of 38 nM. The results would be helpful to design and develop more effective Nek2 inhibitors for the treatment of gastric cancer.

PYRAZOLOPYRIMIDINE DERIVATIVES

The present invention covers Pyrazolopyrimidine compounds of general formula (I), in which n, o, X, Y, R, Q, R1, R2, R3 and R4 are as defined herein, methods of preparing said compounds, intermediate compounds u

PROTEIN KINASE INHIBITORS

A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.

PROTEIN KINASE INHIBITORS

A compound of formula (I), wherein R1 to R5, A, B, Z, Z1 and Z2 are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.

PROTEIN KINASE INHIBITORS

A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.

4, 6-DISUBSTITUTED 2-AMINO-PYRIMIDINES AS HISTAMINE H4 RECEPTOR MODULATORS

The present invention relates to substituted heterocyclic compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.

N-sulfonylanthranilic acid derivatives as allosteric inhibitors of dengue viral RNA-dependent RNA polymerase

A novel class of compounds containing N-sulfonylanthranilic acid was found to specifically inhibit dengue viral polymerase. The structural requirements for inhibition and a preliminary structure-activity relationship are described. A UV cross-linking experiment was used to map the allosteric binding site of the compound on the viral polymerase.