36529-69-8

Upstream product

• 4595-59-9 5-bromopyrimidine 

Downstream Products

• 114969-66-3 5-bromo-4-cyanopyrimidine 
• 38275-57-9 5-bromopyrimidine-2-carbonitrile 

Relevant academic research and scientific papers

From Pyridine- N-oxides to 2-Functionalized Pyridines through Pyridyl Phosphonium Salts: An Umpolung Strategy

The reactions of pyridine-N-oxides with Ph3P under the developed conditions provide an unprecedented route to (pyridine-2-yl)phosphonium salts. Upon activation with DABCO, these salts readily serve as functionalized 2-pyridyl nucleophile equivalents. This umpolung strategy allows for the selective C2 functionalization of the pyridine ring with electrophiles, avoiding the generation and use of unstable organometallic reagents. The protocol operates at ambient temperature and tolerates sensitive functional groups, enabling the synthesis of otherwise challenging compounds.

A safe, convenient and efficient method for the preparation of heterocyclic N-oxides using urea·hydrogen peroxide

A novel, convenient, and high-yielding method has been developed for the preparation of heterocyclic N-oxides. The reaction uses the urea·hydrogen peroxide addition complex as a peroxide source for the in situ generation of trifluoroperacetic acid. The advantages of this method are easy handling of a stable, solid oxidant; high yields and simple removal of excess reagents and by-products.

Substituted piperazines as metabotropic glutamate receptor antagonists

The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, Ar2, Hy, L, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses thereof, processes for making the compounds, as well as methods for the medical treatment of mGluR5-mediated disorders.

METHOD OF PREPARING INHIBITORS OF PHOSPHODIESTERASE-4

In one aspect, the present invention is directed to a one pot method of preparing intermediates of Formula V, which are useful in making inhibitors of phosphodiesterase-4: The present invention is also directed to a method of preparing phosphodiesterase inhibitors comprising the Formula

1-biaryl-1,8-naphthyridin-4-one phosphodiesterase-4 inhibitors

Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterrase 4 inhibitors useful in the treatment of asthma and inflammation.

Studies on Pyrimidine Derivatives. XXXIX. Site-Selectivity in the Reaction of 5-Substituted and 4,5-Disubstituted Pyrimidine N-Oxides with Trimethylsilyl Cynanide

The site-selectivity in the modified Reissert-Henze reaction of 5-substituted and 4,5-disubstituted pyrimidine 1-oxides with trimethylsilyl cyanide was examined.The reaction of 5-substituted 4-methoxypyrimidine 1-oxides with trimethylsilyl cyanide gave exclusively 2-pyrimidinecarbonitriles in good yields without exception.On the other hand, the other 5-substituted and 4,5-disubstituted pyrimidine 1-oxides gave mainly 6-pyrimidinecarbonitriles.Keywords--site-selectivity; pyrimidine N-oxide; trimethylsilyl cyanide; Reissert-Henze reasction; pyrimidinecarbonitrile

Chemistry of Pyrimidine. 2. Synthesis of Pyrimidine N-Oxides and 4-Pyrimidinones by Reaction of 5-Substituted Pyrimidines with Peracids. Evidence for Covalent Hydrates as Reaction Intermediates

The reaction of 5-substituted pyrimidines with peracids has been found to take divergent pathways depending on the presence or absence of a strong acid.Reaction of 5-bromo- (1) or 5-methoxypyrimidine (6) with m-chloroperbenzoic acid afforded the corresponding N-oxides in 29percent and 70percent yields, respectively.The formation of an N-oxide was not observed when either 1 or 6 was treated with 40percent peracetic acid in the presence of 1 equiv of sulfuric acid.In the case of 1, the product was 5-bromo-5(3H)-pyrimidinone (3), formed in 70percent yield.From 6, two products, 5-methoxy-4-(3H)-pyrimidinone (8) and 4(5)-carbomethoxyimidazole (9), were formed in a combined yield of 70percent (3:2 ratio of 8 to 9).The N-oxides were demonstrated to be stable to the above reaction conditions and are therefore not intermediates in the formation of 3, 8, or 9.Evidence for the existence of covalent hydrates makes it reasonable to suggest their formation as reaction intermediates.