Glycine ethyl ester, hydrochloride → Ethyl 2-[(3-amino-5-fluoro-2-pyridinyl)amino]acetate

HRID 466

反応式

HRID 466 の反応式
CCOC(=O)CN.Cl.Nc1cc(F)cnc1Br>CC(=O)O.CC(=O)O.Cc1ccccc1.O=C([O-])[O-].[Cs+].[Cs+].[Pd].c1ccc(P(c2ccccc2)c2ccc3ccccc3c2-c2c(P(c3ccccc3)c3ccccc3)ccc3ccccc23)cc1>CCOC(=O)CNc1ncc(F)cc1N

参加物

7

反応条件

温度
120 °C

実験手順

In a 50 mL round-bottomed flask 2-bromo-5-fluoropyridin-3-amine (500 mg, 2.62 mmol) ethyl 2-aminoacetate hydrochloride (731 mg, 5.24 mmol) BINAP (163 mg, 0.26 mmol) palladium(II) acetate (58.8 mg, 0.26 mmol) CESIUM CARBONATE (2559 mg, 7.85 mmol) were taken.The solids were mixed well and degassed.The toluene was taken in another RB and degassed using Nitrogen.The degassed toluene was then added to the solids.The resulting RM was heated to reflux for 16 hrs. The reaction was monitored by LCMS, which indicated starting material only and no required product. Therefore, the batch was discarded.

出典と根拠

ORDレコード
ord-a7df51f0be0a4af98f3bfe87d6600255
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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