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N-Boc-6-azaindole synthesis

3synthesis methods
-

Yield:370880-82-3 100%

Reaction Conditions:

with triethylamine at 0 - 20; for 3 h;

Steps:

17.1 D/ert-butyl lH-pyrrolo[2.3-c1pyridine-l-carboxylate

To a solution of 6-azaindoIe (6.02 g) and Et3N (14 mL) at 0°C was added (Boc)20 (16.50 mL) dropwise. The reaction mixture was stirred at room temperature for 3 h, washed with water and extracted with EtOAc. The organic layer was dried over anhydrous Na2S04 for 1 h and concentrated in vacuo. The residue was chromatographed with a silica gel column (eluting agent: 3:1 (v/v) PE/EA) to afford the title compound as transparent liquid (11.10 g, 100.00 %). The compound was characterized by the following spectroscopic data: 'HNMR(400 MHz, CDC13) ?: 1.70 (s, 9H), 6.59 (d, J =3.6 Hz, 1H), 7.49 (d, J = 5.3 Hz, 1H), 7.75 (d, .7=3.5 Hz, 1H), 8.40 (d, J= 5.3 Hz, 1H), 9.39 (s, 1H) ppm.

References:

WO2013/71697,2013,A1 Location in patent:Paragraph 00268

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