36216-80-5,A common heterocyclic compound, 36216-80-5,Benzo[d]isoxazol-3-amine, 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.
To a solution of intermediate 3 (0.0025 mol) in isopropylether (5 ml) THF (1 ml) was added and the reaction mixture stirred at RT. Phenylisocyanaat (0.0050 mol) was added and the reaction mixture stirred overnight at RT. The precipitate was filtered off, washed with isopropylether and evaporated dried. The residue was further purified over reversed phase HPLC on a Xterra MS C18 column (3′. 5 Rm, 4.6 x 100 mm) with a flow rate of 1.6 ml/min (Elution conditions: three mobile phases (mobile phase A 95% e t..
25mM ammoniumacetate + 5% acetonitrile; mobile phase B: acetonitrile ; mobile phase C: methanol) were employed to run a gradient condition from 100 % A to 50% B and 50% C in 6.5 min., to 100 % B in 1 min, 100% B for 1 min. and re-equilibrate with 100 % A for 1.5 min.) yielding 0.010 g of compound 4 (yield of 5%, Melting Point 246C)., 36216-80-5
The chemical industry reduces the impact on the environment during synthesis, 36216-80-5,Benzo[d]isoxazol-3-amine,I believe this compound will play a more active role in future production and life.
Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2005/89753; (2005); A2;,
Benzisoxazole – Wikipedia
Benzisoxazole – an overview | ScienceDirect Topics