Sodium cyanoborohydride → tert-butyl 3-({[5-(aminocarbonyl)-1H-imidazol-4-yl]amino}methyl)-4-fluoro-1H-indole-1-carboxylate

참여 물질

반응 단계

A mixture of tert-butyl 4-fluoro-3-formyl-1H-indole-1-carboxylate (1.10 g, 3.0 mmol, obtained from Example 11(a)), 1H-imidazole-5-carboxamide dihydrochloride (0.49 g, 3.0 mmol) and sodium cyanoborohydride (0.38 g, 6.0 mmol) in MeOH (10 mL) was stirred o.n. The reaction mixture was partitioned between H2O (25 mL) and CHCl3 (3×25 mL), the combined organic phase was dried over MgSO4 and evaporated. Purification by flash chromatography using a gradient of MeOH (5-10%) in CHCl3 gave the title compound (0.17 g, 15%). MS (ESI) m/z 374 (M+1).

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