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1-(4-Fluoro-3-nitro-phenyl)-ethanol synthesis

2synthesis methods
-

Yield:774-86-7 90%

Reaction Conditions:

with sodium tetrahydroborate in methanol at 20; for 1 h;

Steps:

138.1

Example 138: Preparation of 2-(2-chIoro-6-fluoro-phenyl)-lH-imidazole-4- carboxylic acid [l-cyclopentyl-5-(l-hydroxy-ethyI)-lH-benzimidazol-2-yl]-amide; Step 1 : Preparation of l-(4-fluoro-3-nitro-phenyl)-ethanol; To a solution of l -(4-fluoro-3-nitro-phenyl)-ethanone (4g, 21,84 mmol) in MeOH added NaBH4 (2.40 g, 3eq), the mixture was stirred for lh at r.t. The mixture was extracted with ethyl acetate and the combined organic layers were dried over MgS04 and concentrated under reduced pressure. Purification by column cliromatography on silica gel (Hex/EA=1/1) to give the title compound: 3.60 g (90%).1H NMR (300 MHz, CDC13) :6(ppm) : 8.10-7.16 (m, 3H) 5.42-5.35 (m, 1H) 1.52 (d, 3H, J= 6.46 HZ)

References:

WO2011/99832,2011,A2 Location in patent:Page/Page column 128-129