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新产品编号:1035137

Chemical Name: 2-[2-Methyl-6-nitro-2-(nitrooxymethyl)-3,4-dihydro-2H-1,4-benzoxazin-4-yl]pyridine 1-oxide
项目整合开发状态: Preclinical
项目研究机构: Yamanouchi (Originator)
合成路线:Treatment of 2-amino-4-nitrophenol (I) with diethyl 2-bromo-2-methylmalonate (II) and KF in DMF provides benzoxazine derivative (III),which is then reduced with BH3-THF complex to yield alcohol (IV).Pyridine N-oxide derivative (VI) is prepared by nucleophilic substitution in (IV) with 2-bromopyridine-N-oxide (V) and NaH in DMF and,finally,(VI) is selectively nitrated with nitronium tetrafluoroborate (NO2BF4) in acetonitrile.
📌 参考资料/链接:
参考文献标题:Novel potassium channel activators.III.Synthesis and pharmacological evaluation of 3,4-dihydro-2H-1,4-benzoxazine derivatives: Modification at the 2 position
文献作者:Matsumoto,Y.; Uchida,W.; Nakahara,H.; Yanagisawa,I.; Shibanuma,T.; Nohira,H.
参考来源:Chem Pharm Bull 2000,48(3),428