反应详情

To a solution of (R)-3-amino-4-(3′-chloro-biphenyl-4-yl)-2-methoxy-butyric acid methyl ester (500 mg, 1.15 mmol) in MeOH (5 mL) is added 2M NaOH aqueous solution (5 mL). After being stirred at room temperature for 2 h, the reaction mixture is acidified with 2M HCl and extracted with EtOAc. The organic layer is dried over Na2SO4 and concentrated. The residue is dissolved in EtOH (5 mL) and treated with SOCl2 (0.252 mL, 3.26 mmol). After being stirred at 55° C., the reaction mixture was cocentrated. The residue is used for a next step without further purification. HPLC retention time=1.49 minutes (condition A): MS (m+1)=348.2

1. extractionextracted with EtOAc
2. dry with materialThe organic layer is dried over Na2SO4
3. concentrationconcentrated
4. dissolutionThe residue is dissolved in EtOH (5 mL)
5. stirringAfter being stirred at 55° C.
6. customThe residue is used for a next step without further purification