(S)-tert-butyl 2-phenylmorpholine-4-carboxylate synthesis

Yield:-

Reaction Conditions:

with triphenylphosphine;diethylazodicarboxylate in toluene at 20;

Steps:

2

(S)-2-Phenyl-morpholine-4-carboxylic acid tert-butyl ester; 3g of (S)-(2-Hydroxy-ethyl)-(2-hydroxy-2-phenyl-ethyl)-carbamic acid tert-butyl ester and 0.327g of triphenylphosphine were dissolved in 53.3mL toluene. 0.217g of diethylazodicarboxylate in 5.4mL toluene was added dropwise to the resulting solution at room temperature under argon atmosphere and the mixture was stirred overnight. The solvent was removed in vacuo and the material purified by column chromatography.

References:

WO2007/70760,2007,A2 Location in patent:Page/Page column 19