APCP-363, APO-363

Chemical Name: 3-Hydroxy-2-(1-methoxyethyl)-1,6-dimethyl-1,4-dihydropyridin-4-one
CAS No. 216581-37-2 (hydrochloride)
项目整合开发状态: Preclinical
项目研究机构: BTG (Originator), Apotex (Licensee)
合成路线:Treatment of allomaltol (I) with acetaldehyde (II) and NaOH in H2O affords pyranone derivative (III),which is benzylated by means of benzyl bromide (IV) and NaOH in refluxing H2O/MeOH to provide compound (V).O-Methylation of (V) by reaction with NaH and MeI in DMF furnishes methoxyethyl derivative (VI),which is then heated with methylamine and NaOH in EtOH/H2O to yield pyridinone derivative (VII).Finally,the benzyl group of (VII) is removed by hydrogenation over Pd/C in MeOH to give the desired product.