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5-NITRO-2-PIPERIDINOBENZALDEHYDE synthesis

3synthesis methods
-

Yield:30742-60-0 94%

Reaction Conditions:

with N-ethyl-N,N-diisopropylamine in N,N-dimethyl-formamide at 20;

Steps:

136.1 5-nitro-2-(piperidin-1-yl)benzaldehyde:

2-fluoro-5-nitrobenzaldehyde (1 g, 5.91 mmol) wasdissolved in DMF (10 mL) and piperidine (0.64 mL, 6.50 mmol) was added, followed by DIPEA (2.27 mL, 13.0 mmol) The mixture was stirred overnight at room temperature. Water was added and the resulting precipitate was collected by filtration and dried in vacuo to give thetitle compound (1.3 g, 94%) as a yellow solid which was used without further purification. LCMS (Method C) : =1.59 mm, m/z = 235 [M+H].

References:

WO2015/92431,2015,A1 Location in patent:Page/Page column 266; 267

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