79691-74-0

Usage

Uses

Used in Pharmaceutical Industry:
5-Pyrimidinemethanol, alpha-methyl(9CI) is used as a key intermediate in the synthesis of muscarinic agonists for the treatment of Alzheimer's disease. As a pyrimidine derivative, it plays a crucial role in the development of these drugs, which aim to improve cognitive function and memory in patients suffering from this neurodegenerative disorder.

Upstream product

• 75-16-1 methylmagnesium bromide 
• 10070-92-5 pyrimidine-5-carbaldehyde 
• 60025-05-0 4,6-dichloro-5-(α-hydroxyethyl)pyrimidine 

Downstream Products

• 10325-70-9 1-(pyrimidin-5-yl)ethan-1-one 
• 591-55-9 pyrimidin-5-amine 

Relevant academic research and scientific papers

cGAS ANTAGONIST COMPOUNDS

Disclosed are novel compounds of Formula (I) that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.

Synthesis and muscarinic activity of 1,2,3,4-tetrahydropyrimidine derivatives

3-Methyl-1,2,3,4-tetrahydropyrimidine-5-carbaldehyde O-substituted oximes 4 and 1-(3-methyl-1,2,3,4-tetrahydropyrimidin-5-yl)ethanone O-substituted oximes 9 have been prepared as bioisosteric congeners of arecoline which is a muscarinic agonist for treatment of Alzheimer's disease. Starting from pyrimidine-5-carbaldehyde 1, formation of the 3-methylpyrimidinium salt and subsequent reduction afforded 1,2,3,4-tetrahydropyrimidine derivatives which were converted into oxalate salts in the interest of purity and stability. Binding affinities of prepared compounds for the cloned human muscarinic M1 receptor (h-M1) were determined by radioligand binding assay using [3H]-N-methylscopolamine (NMS).

Pyridocarbazole derivatives having cGMP-PDE inhibitory activity

PCT No. PCT/JP97/01829 Sec. 371 Date Jan. 29, 1998 Sec. 102(e) Date Jan. 29, 1998 PCT Filed May 29, 1997 PCT Pub. No. WO97/45427 PCT Pub. Date Dec. 4, 1997The invention relates to novel pyridocarbazole derivatives having highly selective action in inhibiting cyclic GMP-phosphodiesterase (hereinafter abbreviated as cGMP-PDE), processes for producing such derivatives, agents containing at least one of such derivatives as an active ingredient for preventing and/or treating pulmonary hypertension, ischemic heart diseases or diseases against which the cGMP-PDE inhibitory action is effective, and intermediates useful for the production of pyridocarbazole derivatives.

PYRIMIDINES. 73. SYNTHESIS OF ACETYLPYRIMIDINES

It is shown that the use of benzene as the solvent in the preparation of 2- and 4-acetylpyrimidines from cyanopyrimidines via the Grignard reaction makes this reaction a practical method for the preparation of pyrimidinyl ketones.Preparatively convenient methods for the preparation of 4-acetylpyrimidine from 4-ethylpyrimidine through the α-oximino derivative and 5-acetylpyrimidine from 4,6-dichloro derivatives of pyrimidine are proposed.