反応 #155354

ord-09aa0f18d178482db1ba08d7c1f7198a

反応方程式

CCOC(C)=O.Cl
hydrogen chloride ethylacetate
CCCOc1ccc(F)c2c(=O)c(-c3ccc(OC)cc3)cn(COP(=O)(OC(C)(C)C)OC(C)(C)C)c12
di-tert-butyl 5-fluoro-3-(4-methoxyphenyl)-4-oxo-8-propoxy-4H-quinolin-1-ylmethyl phosphate
CCCOc1ccc(F)c2c(=O)c(-c3ccc(OC)cc3)cn(CCl)c12
1-chloromethyl-5-fluoro-3-(4-methoxyphenyl)-8-propoxy-1H-quinolin-4-one
収率 92.0%

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    温度cooling
  2. 2
    ろ過The deposited insoluble matter was collected by filtration
  3. 3
    その他dried

実験手順

A 4N hydrogen chloride ethylacetate solution (2 ml) was added to an ethyl acetate solution (3 ml) of di-tert-butyl 5-fluoro-3-(4-methoxyphenyl)-4-oxo-8-propoxy-4H-quinolin-1-ylmethyl phosphate (300 mg, 0.55 mmol) while ice-cooling and the mixture was stirred at room temperature for 2 hours. The deposited insoluble matter was collected by filtration and dried, giving a white powder of 1-chloromethyl-5-fluoro-3-(4-methoxyphenyl)-8-propoxy-1H-quinolin-4-one (18 mg, yield: 92%).

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: USRE045108E1uspto-grants-2014_09