2-Amino-1-(4-nitrophenyl)-1,3-propanediol synthesis

Yield:119-62-0 91.1%

Reaction Conditions:

with hydrogenchloride in lithium hydroxide monohydrate at 100;

Steps:

1.1.S10 S10. Preparation of intermediate 15

Chloramphenicol, compound 14 (25 g, 77.6 mmol) in HCl (1 M, 500 mL), was stirred at 100 °C overnight. LC-MS showed the reaction was complete. The reaction solution was cooled to room temperature and extracted with ethyl acetate (EA) (500 mL×3) to remove dichloroacetic acid. The remaining aqueous phase was spin-dried to obtain a white solid of chloramphenicol hydrolyzate, chloramphenicolamine (CAPA), intermediate 15 (15 g, yield: 91.1%, 70.7 mmol).

References:

CN114539171,2022,A Location in patent:Paragraph 0043-0044; 0072-0074