With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.81282-60-2,7-Aminobenzo[d]oxazol-2(3H)-one,as a common compound, the synthetic route is as follows.
A solution of Ms20 (32 1 g, 184.8 mmol) in MeCN (200 mL) was cooled to < -5 C (ice/H20 salt) and sequentially were added a solution of N-benzyl-bis(2- hydroxyethyl)amine (16.4 g, 84.1 mmol) in MeCN (50 mL), Et3N (36 mL, 255 mmol, 3.8 eq.), and MsOH (13.1 mL, 202 mmol, 3 eq.) while maintaining the temperature below 10C. 7-Aminobenzo[d]oxazol-2(3H)-one (10.0 g, 67.2 mmol) was added as a solid and the mixture was heated to reflux. Et3N (28.5 mL, 202 mmol) was added drop- wise over a period of 1.5 hour. Reflux was maintained for 18 additional hours. The resulting clear solution was allowed to cool to RT and concentrated in vacuo at 70C. The residue was separated between NaHCC (0.8 L) and EtOAc (0.4 L). The aqueous layer was extracted with EtOAc (3 x 0.2 L). The combined organic layers were washed with brine, dried (NaiSC^) and concentrated to afford 7-(4-benzylpiperazin-l- yl)benzo[d]oxazol-2(3H)-one as a white solid (20.2 g, 65.3 mmol, 97%).
81282-60-2 7-Aminobenzo[d]oxazol-2(3H)-one 11147814, abenzoxazole compound, is more and more widely used in various.
Reference£º
Patent; AAPA B.V.; HEERES, Andre; WILLIGERS – HOGG, Sandra; BORST, Marcus Leonardus Gerardus; DROeGE, Melloney Joyce; WO2015/69110; (2015); A1;,
Benzoxazole – Wikipedia
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