On December 30, 1987, Uno, Hitoshi; Kurokawa, Mikio; Sato, Fiminori; Naruto, Shunsuke; Masuda, Yoshinobu published a patent.Synthetic Route of 114312-57-1 The title of the patent was Processes for the preparation of 11-piperazinyl-6,11-dihydrodibenz[b,e]oxepins as antianoxia agents. And the patent contained the following:
Title compounds I [R1 = H, MeO; R2 = H, MeO, HO, F; R3 = H, F; R4 = H, 7-, 8-, 9-F; Ar = Ph, thienyl, pyridyl] and their physiol. acceptable salts are prepared from II [R1, R3, R4 = same as I; R2 = H, MeO, (protected) HO, F, reactive ester residue (O is attached to the rings)] and III (Ar = same as I). (E)-III (Ar = Ph) (4.0 g) was treated with 2.0 g II (R1 = R2 = R4 = H, R3 = F, Y = Cl) (preparation given) in CHCl3 at room temperature for 2 h to give 1.5 g (E)-I (R1 = R2 = R4 = H, R3 = F, Ar = Ph), which was converted into the maleate salt monohydrate (IV). IV showed cerebral antianoxia activity at min. ED of 10 mg/kg p.o. in ischemic mice and life-prolongation activity for anoxia at 100 mg/kg in mice, vs. > 100 mg/kg p.o. and no life-prolongation activity, resp., for I (R1 = R2 = R4 = H, R3 = Me, Ar = Ph) dioxalate hydrate (V). A film-coated tablet containing IV 5, corn starch 33, lactose 75, cellulose 30, hydroxypropylcellulose 5, SiO2 1, and Mg stearate 1 g was prepared The experimental process involved the reaction of Ethyl 3-fluoro-2-methylbenzoate(cas: 114312-57-1).Synthetic Route of 114312-57-1
The Article related to piperazinyl dihydro dibenzoxepin preparation antianoxia, dibenzoxepin piperazinyldihydro preparation antianoxia, oxepin piperazinyldihydrodibenzoxepin preparation antianoxia and other aspects.Synthetic Route of 114312-57-1
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