Piperazine → 4-Fluoro-2-(piperazin-1-yl)benzonitrile

HRID 318

反応式

HRID 318 の反応式
C1CNCCN1.N#Cc1ccc(F)cc1Br>C1COCCO1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C([O-])[O-].[Cs+].[Cs+].[Pd].[Pd].c1ccc(P(c2ccccc2)c2ccc3ccccc3c2-c2c(P(c3ccccc3)c3ccccc3)ccc3ccccc23)cc1>N#Cc1ccc(F)cc1N1CCNCC1

参加物

7

反応条件

温度
90 °C

実験手順

Tris(dibenzylideneacetone)dipalladium (0) (57.2 mg, 0.06 mmol) and rac-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (78 mg, 0.12 mmol) were added to a mixture of 2-bromo-4-fluorobenzonitrile (250 mg, 1.25 mmol), Cesium carbonate (611 mg, 1.87 mmol) and Piperazine (215 mg, 2.50 mmol) in dioxane (3 mL). Reaction vessel was placed in an oil bath at 90 °C 4pm. LCMS o/n shows several peaks. Larger peak corresponding to displacement of F by piperazine (MW266) than for desired product (205). Discarded

出典と根拠

ORDレコード
ord-91c1aa5c02fc46a586e9f5a373b7526a
出典データセット
750 AstraZeneca ELN dataset
元リンク
出典を表示

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