857641-46-4

Usage

Uses

Used in Pharmaceutical Industry:
2-(4-BROMO-1H-PYRAZOL-1-YL)PYRIMIDINE is used as a building block for the synthesis of various biologically active compounds. Its unique structure and reactivity contribute to the development of new pharmaceuticals with potential therapeutic applications.
Used in Agrochemical Industry:
In the agrochemical industry, 2-(4-BROMO-1H-PYRAZOL-1-YL)PYRIMIDINE serves as a key intermediate in the production of agrochemicals. Its properties and functional groups enable the creation of new compounds with potential applications in agriculture, such as pesticides and herbicides.
Used in Medicinal Chemistry and Drug Discovery:
2-(4-BROMO-1H-PYRAZOL-1-YL)PYRIMIDINE is utilized as a valuable intermediate in medicinal chemistry and drug discovery. Its diverse properties and functional groups make it a promising candidate for the development of new drugs and therapeutic agents.

InChI:InChI=1/C7H5BrN4/c8-6-4-11-12(5-6)7-9-2-1-3-10-7/h1-5H

Upstream product

• 2075-45-8 4-bromo-1H-pyrazole 
• 1722-12-9 2-chloropyrimidine 
• 82882-56-2 1-(pyrimidin-2-yl)-1H-pyrazole 

Downstream Products

• 1312940-07-0 propane-1-sulfonic acid {2,4-difluoro-3-[5-(1-pyrimidin-2-yl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amide 
• 857641-50-0 [Pd(η3-C4H7)(2-(4-bromo-1H-pyrazol-1-yl)pyrimidine)][tetrakis(3,5-trifluoromethylphenyl)borate] 

Relevant academic research and scientific papers

Imidazopyridazines as potent inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1): Preparation and evaluation of pyrazole linked analogues

The structural diversity and SAR in a series of imidazopyridazine inhibitors of Plasmodium falciparum calcium dependent protein kinase 1 (PfCDPK1) has been explored and extended. The opportunity to further improve key ADME parameters by means of lowering log D was identified, and this was achieved by replacement of a six-membered (hetero)aromatic linker with a pyrazole. A short SAR study has delivered key examples with useful in vitro activity and ADME profiles, good selectivity against a human kinase panel and improved levels of lipophilic ligand efficiency. These new analogues thus provide a credible additional route to further development of the series.

HETEROCYCLIC COMPOUNDS AND USE THEREOF AS ERK INHIBITORS

Disclosed are the ERK inhibitors of formula 1.0: [Formula (1.0)] and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

POLYCYCLIC INDAZOLE DERIVATIVES AND THEIR USE AS ERK INHIBITORS FOR THE TREATMENT OF CANCER

Disclosed are the ERK inhibitors of formula 1.0: (Chemical formula should be inserted here as it appears on abstract in paper form) and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

Apparent allyl rotation and Pd-N bond rupture in allylpalladium complexes with N-donor ligands - Evidence of an associative mechanism

The new didentate N-donor ligands 2-(4-methyl-1H-pyrazol-1-yl)pyrimidine (4Me-pzpm, 1) and 2-(4-bromo-1H-pyrazol-1-yl)pyrimidine (4Br-pzpm, 2) have been synthesised and used to obtain the allylpalladium derivatives [Pd(η3-2Me-C3H4)(NN′)]X [X = BAr′4-, NN′ = 1 (3), NN′ = 2 (4); X = CF3SO3-, NN′ = 1 (5), NN′ = 2 (6)]. In complexes 3-6 two types of fluxional process have been found: apparent allyl rotation that is observed as Hsyn-Hsyn, H anti-Hanti interconversions and H4-H 6 interchange of the pyrimidine protons that must involve Pd-N(pm) bond rupture. The influence of different factors on both processes - such as the nature of the N-donor ligand, counterion, solvent, complex concentration and addition of water - has been studied. It has been concluded that the apparent allyl rotation has a lower free energy of activation and in both cases the presence of a species with coordinating ability favours the process. Negative entropies of activation have been found. Associative mechanisms involving participation of five-coordinate intermediates have been proposed. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005.