Reaktion #588429

Reaktionsgleichung

NaHCO3

methyl 4-fluoro-5-methanesulfonyl-2-methylbenzoate

4-phenyl-isothiazolidine 1,1-dioxide

Cs2CO3

→

colorless oil

Ausbeute 83.8%

Methyl 4-(1,1-dioxo-4-phenylisothiazolidin-2-yl)-5-methanesulfonyl-2-methylbenzoate

Ausbeute 83.8%

Lösungsmittel

DMF

Reaktionsbedingungen

Aufarbeitung

1. 1
   Extraktionextracted 3 times with 140 ml of EA each time
2. 2
   TrocknenAfter drying over Na2SO4
3. 3
   Sonstigethe solvent was removed in vacuo

Vorschrift

600 mg of methyl 4-fluoro-5-methanesulfonyl-2-methylbenzoate (Journal of Medicinal Chemistry (1997), 40(13), 2017), 600 mg of 4-phenyl-isothiazolidine 1,1-dioxide (Pharmaceutical Chemistry Journal (Translation of Khimiko-Farmatsevticheskii Zhurnal) (2000), Volume Date 1999, 33(11), 598) and 2.379 g of Cs2CO3 were stirred in 20 ml of anhydrous DMF at RT for 4 hours. The reaction mixture was then poured into 220 ml of a half-saturated aqueous NaHCO3 solution and extracted 3 times with 140 ml of EA each time. After drying over Na2SO4, the solvent was removed in vacuo. Chromatography on silica gel with DIP afforded 865 mg of a colorless oil.

Quelle