Methyl chloroformate → (S)-(1-{4-[4-(4-Ethoxy-phenyl)-piperidin-1-yl]-phenyl}-ethyl)-carbamic acid methyl ester

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Reaction Steps

To a mixture of 36.1 mg (0.10 mmol) (S)-1-{4-[4-(4-ethoxy-phenyl)-piperidin-1-yl]-phenyl}-ethylamine hydrochloride (XII.1) and 42.7 μL (0.250 mmol) DIPEA in 2 mL THF are added 11.64 (0.150 mmol) methyl chloroformate at 0° C. The mixture is stirred for 12 h at rt. The solvent is removed under reduced pressure, the residue is taken up in DMF and purified by HPLC (Sunfire, narrow gradients, water (+0.1% TFA)/methanol) to yield the desired product.

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