On January 5, 2021, Li, Yanxiong; Meng, Faming; Xu, Liang; Guo, Jun published a patent.Formula: C9H11NO2 The title of the patent was Preparation method of aprepitant intermediate (2R,3R)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholine. And the patent contained the following:
The title preparation method includes mixing compound I ((R)-6-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-5-(4-fluorophenyl)-3,6-dihydro-2H-1,4-oxazine), chiral catalyst, acid (protonic acid such as trifluoroacetic acid, acetic acid, etc.) and solvent (chloroform, dichloromethane, etc.) for reaction to obtain the final aprepitant intermediate (2R,3R)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholine (compound II). The chiral catalyst is compound including bis((S)-2-amino-2-oxo-1-phenylethyl) 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, bis((S)-2-(methylamino)-2-oxo-1-phenylethyl) 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, etc. The invention has high yield and product purity, and is environment-friendly. The experimental process involved the reaction of (S)-2-Hydroxy-N-methyl-2-phenylacetamide(cas: 65645-88-7).Formula: C9H11NO2
The Article related to aprepitant intermediate preparation, morpholine fluorophenyl preparation, Heterocyclic Compounds (More Than One Hetero Atom): Oxazines (Including Morpholine) and other aspects.Formula: C9H11NO2
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics