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2-Nitro-5-(piperidin-1-yl)benzaMide synthesis

7synthesis methods
-

Yield:421558-77-2 100%

Reaction Conditions:

with N-ethyl-N,N-diisopropylamine in tetrahydrofuran at 70; for 12 h;Heating / reflux;

Steps:

I.18.B Step B : 2-nitro-5-piperidin-1-yl-benzamide

[00362] To 5-FLUORO-2-NITRO-BENZAMIDE (850mg, 4. 07MMOL) in THF (LOOML), was added piperdine (381mg, 4. 47MMOL) and diisopropyl ethyl amine (780 ML, 4.07mmol) and the solution was heated to 70 C in a sealed tube for 12h. The resulting yellow precipitate was collected to give 2-Nitro-5-piperidin-1-yl-benzamide 948mg (100% yield) HPLC tr=3. 58min (100%), FIA m/e 250.2 (M+H) 248.8 (M-H); HNMR (500 MHz, dmso): 6 7.95 (lH, d), 7.85 91H, bs), 7.50 (1H, bs), 6.97 (LH, d), 6.80 (1H, s), 3.50 (4H, m), 1.70-1. 50 (6H, m).

References:

WO2004/37814,2004,A1 Location in patent:Page 177