With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4570-41-6,Benzo[d]oxazol-2-amine,as a common compound, the synthetic route is as follows.
Step 5:To a solution of (S)-2-(4-methanesulfonyl-phenyl)-3-o-tolyl-propionic acid (214 mg, 0.67 mmol) and 2-amino-benzoxazole (90 mg, 0.67 mmol) in CH2Cl2 (10 mL) was added DMAP (24 mg, 0.2 mmol) and EDC.HCl (154 mg, 0.8 mmol).The reaction mixture was stirred at room temperature for 2 days.The reaction mixture was concentrated in vacuo.Purification by chromatography (silica, 0-1.5percent methanol/CH2Cl2 gradient), followed by RPHPLC purification (C4 reverse phase, 10-90percent acetonitrile/0.1percent aqueous TFA buffer) afforded (S)-N-Benzooxazol-2-yl-2-(4-methanesulfonyl-phenyl)-3-o-tolyl-propionamide (68 mg, 23percent): m.p. 106-108¡ã C., LC/MS-ESI observed [M+H]+ 435, [alpha]28=+43.6¡ã (c=0.5, methanol), 75percent ee by chiral HPLC determination.
The synthetic route of 4570-41-6 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; Brotherton-Pleiss, Christine E.; Walker, Keith A. M.; US2012/149718; (2012); A1;,
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