3-甲氧基-4-(4-甲基-1H-咪唑-1-基)苯胺 → (R)-N-(3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl)-6-methyl-8-phenyl-5,6,7,8-tetrahydropyrimido[5,4-f][1,4]oxazepin-2-amine

HRID 270

反应方程式

HRID 270 反应方程式
CN1Cc2cnc(Cl)nc2O[C@H](c2ccccc2)C1.COc1cc(N)ccc1-n1cnc(C)c1>C1COCCO1.CC(=O)O.CC(=O)O.CC(C)(C)P(C(C)(C)C)C(C)(C)C.CCC(C)(C)[O-].[Na+].[Pd]>COc1cc(Nc2ncc3c(n2)O[C@H](c2ccccc2)CN(C)C3)ccc1-n1cnc(C)c1

参与物

7

反应物 2

HCID 454801813-甲氧基-4-(4-甲基-1H-咪唑-1-基)苯胺HCID 59577867(R)-2-chloro-6-methyl-8-phenyl-5,6,7,8-tetrahydropyrimido[5,4-f][1,4]oxazepine

产物 1

HCID 49820859(R)-N-(3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl)-6-methyl-8-phenyl-5,6,7,8-tetrahydropyrimido[5,4-f][1,4]oxazepin-2-amine收率 0%

试剂、催化剂与溶剂 4

HCID 2733478叔戊醇钠试剂HCID 83681三叔丁基膦催化剂HCID 4144353醋酸钯催化剂HCID 312751,4-二氧六环溶剂

反应条件

温度
120 °C

实验过程

(R)-2-chloro-6-methyl-8-phenyl-5,6,7,8-tetrahydropyrimido[5,4-f][1,4]oxazepine (0.05 g, 0.18 mmol), PALLADIUM(II) ACETATE (1.221 mg, 5.44 µmol) (1.6), 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline (0.037 g, 0.18 mmol) (0.64), Tri-tert- butylphosphonium tetrafluoriborate (0.0043 g, 0.014 mmol, 6 mol%) and Na-t-amilate (0.022 g, 1.1 equ, 0.2 mmol) in 1 ml of dioxane was degaset over argone and heated in MW 120°C 30 min. No reaction. Experiment was not progressed.

来源与证据

ORD记录
ord-3a2eb97137e148aba58c08979aa7d29e
来源数据集
750 AstraZeneca ELN dataset
原始链接
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