HRID1524240

反应详情

EQUATION

反应方程式

HRID 1524240 的结构方程式

AUXILIARIES

试剂、催化剂与溶剂

1

CONDITIONS

反应条件

温度
150 °C

PROCEDURE

实验过程

A mixture of (tert-butoxy)-N-(5-bromo(1,3-thiazol-2-yl)carboxamide (52, 140 mg, 0.5 mmol), 1-methylindol-2-yl boronic acid (88 mg, 0.5 mmol), [1,1′-bis(diphenylphosphino)ferrocene]palladium(II) chloride dichloromethane complex (1:1) (40 mg) and potassium phosphate (106 mg) in 2 ml DMF and 0.5 ml water was heated under Ar in microwave reactor at 150° C. for 30 min. The reaction mixture was worked up with EA/brine. Org. phase was concentrated and then subjected to silica gel flash column purification (0-100% B, A: hexane; B: EA) to give 21 mg 5-(1-methylindol-2-yl)-1,3-thiazole-2-ylamine (53) as brown solid (yield: 18.3%; purity>90%).

WORKUP

后处理

  1. concentrationphase was concentrated
  2. customsubjected to silica gel flash column purification (0-100% B