4-[[(1R)-3-(4-Morpholinyl)-1-[(phenylthio)methyl]propyl]amino]-3-[(trifluoromethyl)sulfonyl]benzenesulfonamide → (R)-(4'-chlorobiphenyl-2-yl)(1-(4-(4-((R)-4-morpholino-1-(phenylthio)butan-2-ylamino)-3-(trifluoromethylsulfonyl)phenylsulfonylcarbamoyl)phenyl)piperidin-4-yl)methyl methyl hydrogen phosphate, hydrochloride salt

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A mixture of (R)-4-(4-((4′-chlorobiphenyl-2-yl)(dimethoxyphosphoryloxy)methyl)piperidin-1-yl)benzoic acid (INTERMEDIATE 122, 57.4 mg, 0.11 mmol), (R)-4-(4-morpholino-1-(phenylthio)butan-2-ylamino)-3-(trifluoromethylsulfonyl)benzenesulfonamide (INTERMEDIATE 69, 60 mg, 0.11 mmol), EDC (41.6 mg, 0.22 mmol), TEA (0.03 ml, 0.22 mmol), and DCE (2 ml) were stirred at r.t. for 4 days. The volatiles were removed under reduced pressure and the concentrate was purified by reverse phase HPLC according to the following conditions:

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