87591-84-2

Usage

Uses

Used in Pharmaceutical Industry:
2-CHLOROMETHYL-8-METHYL-PYRIDO[1,2-A]PYRIMIDIN-4-ONE is used as a key intermediate in the synthesis of various pharmaceutical compounds. Its unique structural features and functional groups allow for the development of new drugs with potential therapeutic applications.
Used in Medicinal Chemistry Research:
In the field of medicinal chemistry, 2-CHLOROMETHYL-8-METHYL-PYRIDO[1,2-A]PYRIMIDIN-4-ONE serves as a valuable building block for the design and synthesis of novel bioactive molecules. Its chemical properties make it suitable for further modification and optimization to enhance the potency, selectivity, and pharmacokinetic properties of drug candidates.
Used in Drug Discovery:
2-CHLOROMETHYL-8-METHYL-PYRIDO[1,2-A]PYRIMIDIN-4-ONE is utilized in drug discovery processes to identify and develop new therapeutic agents. Its potential biological activity and chemical versatility make it an attractive candidate for high-throughput screening and lead optimization efforts aimed at discovering innovative treatments for various diseases and conditions.

InChI:InChI=1/C10H9ClN2O/c1-7-2-3-13-9(4-7)12-8(6-11)5-10(13)14/h2-5H,6H2,1H3

Upstream product

• 695-34-1 2-Amino-4-methylpyridine 
• 638-07-3 ethyl (2-chloroaceto)acetate 

Relevant academic research and scientific papers

A radical synthetic approach to the new potentially bioactive pyrimidinones

2-Chloromethyl-8-methyl-3-nitro-4H-pyrido[1,2-a]pyrimidin-4-one was shown to react with various nitronate or malonate anions under mild conditions to give potentially bioactive nitro-4H-pyrido[1,2-a]pyrimidin-4-ones. Extension to other anions centred on S

Preparation and synthesis method of aromatic amine compound with function of specifically inhibiting HIF-2alpha

The invention relates to a preparation method of an HIF-2alpha small-molecule inhibitor (2-((benzyl(furan-2-yl methyl) amino) methyl)-8-methyl-4H-pyrido[1, 2-a]pyrimidine-4-ketone). The compound is characterized in that 4-methylpyridine-2-amine is used as an initial raw material, and 2-chloro-8-methyl-4H-pyrido [1, 2-a] pyrimidine-4-ketone is obtained through condensation cyclization of 4-methylpyridine-2-amine and the compound, furfural is taken as an initial raw material, an addition reaction is carried out on the furfural and benzylamine to obtain N-furan benzylamine, and a N-alkylation reaction is carried out on the obtained 2-chloro-8-methyl-4H-pyrido[1, 2-a]pyrimidine-4-ketone and N-furan benzylamine to obtain the HIF-2alpha small-molecule inhibitor. The invention discloses the preparation method of the HIF-2alpha small-molecule inhibitor for the first time, the method has the advantages of few steps, simple operation, rapid reaction and no need of high pressure, the yield and purity of the prepared compound are high, and the raw materials are easy to obtain.

Synthesis and antiproliferative activitiy of novel diaryl ureas possessing a 4H-pyrido[1,2-a]pyrimidin-4-one group

We herein disclose a series of novel diaryl urea derivatives possessing a 4H-pyrido[1,2-a]pyrimidin-4-one group as novel potent anticancer compounds. The structures were confirmed by IR, 1H-NMR, and MS. All the compounds were screened for their antiprofilerative activity agaist the human breast cancer cell line (MDA-MB-231). The pharmacological results indicated that most of the compounds showed moderate activity. The best of this series is compound 4c (IC50 = 0.7 μmol/L), with a potency 3.6-fold higher than Sorafenib (IC50 = 2.5 μmol/L), which was approved in 2005.

Synthesis of some substituted pyrido[1,2-a]pyrimidin-4-ones and 1,8-naphthyridines

The substituted 4H-pyrido[1,2-a]pyrimidin-4-ones (I) were obtained by the condensation of substituted 2-aminopyridines with β-ketocarboxylic esters in PPA. Some of the derivatives I were transformed into the corresponding 1,8-naphthyridines II and III.