4-Chloro-3-(methanesulfonylmethyl)aniline → 5-[4-Chloro-3-(methylsulfonylmethyl)anilino]-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile

HRID 670

反応式

HRID 670 の反応式
CS(=O)(=O)Cc1cc(N)ccc1Cl.N#Cc1cnn2c(NC3CC3)cc(Cl)nc12>CC(=O)N(C)C.CC1(C)c2cccc(P(c3ccccc3)c3ccccc3)c2Oc2c(P(c3ccccc3)c3ccccc3)cccc21.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]>CS(=O)(=O)Cc1cc(Nc2cc(NC3CC3)n3ncc(C#N)c3n2)ccc1Cl

参加物

7

反応条件

温度
150 °C

実験手順

In a 40mL vial (t=g) was 5-chloro-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile (88 mg, 0.38 mmol), [Reactants], and cesium carbonate (135 mg, 0.41 mmol) in DMA (0.5 mL) ([VOLUME]),Pd2(dba)3 (17.24 mg, 0.02 mmol) and (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (21.79 mg, 0.04 mmol) were added. to give a brown suspension. The vial was filled with N2, 150C microwave for 30 min. LCMS showed completion. added DMF(3 mL), filtered through celite. concentrated. The residue was washed with EtOAc and water, MeoH to give about 55mg light brown solid

出典と根拠

ORDレコード
ord-31892db8bbd04de79164da0921726b58
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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