Ethyl 3-((R)-((R)-1,1-dimethylethylsulfinamido)(phenyl)methyl)phenyl(methyl)phosphinate → Ethyl 3-((R)-amino(phenyl)methyl)phenyl(methyl)phosphinate

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Reaction Steps

Ethyl 3-((R)—((R)-1,1-dimethylethylsulfinamido)(phenyl)methyl)phenyl(methyl)phosphinate, 24-d, (15 g, 80% purity, 32.3 mmol) was dissolved in HCl/dioxane (70 ml, 4 mol/L) and the mixture was stirred at room temperature for 2 h. The mixture was concentrated under vacuum and the residue was dissolved with H2O (90 ml) and HCl (10 ml). The aqueous phase was extracted with EA (80 ml*5). The pH of the aqueous layer was adjusted to about pH=12 and extracted with EA (100 ml*3). The organic was dried over Na2SO4 and the crude product was purified with column (DCM/MeOH=100/1˜30/1) to provide the product, 24-e, (6.77 g, 74%).

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