Application of 722-92-9 ,Some common heterocyclic compound, 722-92-9, molecular formula is C9H7F6NO, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.
Intermcdiate H; 6-Chloro-3-(2-ethoxy-3,4-dioxo-cyclobut- 1 -enylamtno)-2-hydroxy-N-(4-{2,2,2-trif luoro-1 – hydroxy-l-triftuoromepsilonthyl-ethyl)-phenylj-benzenesulfonamide; HIi Preparation of Intermediate Ht; 2-rert-Butyl-6-chloro-ben*zooxazole-7-sul-:onic acid [4-{2,2,2-trifluoro-l -hydroxy-1 -trifluoromethyl-ethy I )~rhohenyl]-amide; 2-tert-Buryl-6-chJoro-ben20oxazole-7-sulfonyl chloride (500 mg, 1.62 mmo.) {prepared according to the procedure described in US 2007/067088 page 17} , 2-(4-aminophenyl)- l,l,l,3,3,3-hexafluoropropan-2-ol (420 mg, 1.62 mmol) and triethylamine (0.226 ml, 1.62 mmol) were combined in THF (5 ml) to give a yellow solution. The reaction, mixture was stirred at room temperature for 2 h then heated at 50 0C for 48 h. The reaction mixture was partitioned between EtOAc (20 ml) and IM HCI (10 ml), live organic layer was washed with brine (10 ml), dried (MgSO-O, filtered and added to silica gel (4 g) then carefully evaporated in vacuo. The silica gel was dry-loaded onto an (Isolure.(TM). Flash Si II 25 g) column for purification by chromatography, eluting with iso-hexane/ErOAc (10/1). The product fractions were combined and evaporated to dryness in vacuo to yield the title product. IH NMR 6H (400MHz DMSO) 8.55 (s, IH), 7.94 (d, IH), 7.61 (d, IH), 7.49 (d, 2H) 7.19
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