1-Ethyl-3-piperidinol → Trifluoroacetic acid

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A mixture of N-{4-[2-chloro-6-(4-trifluoromethyl-phenyl)-pyrimidin-4-yloxy]-benzo[d]thiazol-2-yl}-acetamide (70 mg, 0.15 mmol, Example 7(d)) and 1-ethyl-3-hydroxypiperidine (39 mg, 0.3 mmol, Aldrich) in ethanol (1 mL) was heated in a microwave synthesizer at 140° C. for 20 min. The reaction mixture was diluted with sat. aqueous solution of NaHCO3 (10 mL) and extracted with EtOAc (2×30 mL). The combined organic extracts were washed with brine (20 mL), dried over Na2SO4, and filtered. The filtrate was concentrated in vacuo and the residue was purified by preparative HPLC [gradient 20-80% MeCN (0.1% TFA)/H2O (0.1% TFA)] to give the title compound as a salt with TFA. MS (ESI, pos. ion) m/z: 516 (M+1).

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