HRID1744127
反应详情
EQUATION
反应方程式
REACTANTS
反应物
PRODUCTS
生成物
AUXILIARIES
试剂、催化剂与溶剂
PROCEDURE
实验过程
To N-(4-{4-[4-(tert-butoxycarbonyl)piperazin-1-yl]phenyl}-1,2,5-oxadiazol-3-yl)leucine (350 mg, 0.763 mmol), PyBOP (440 mg, 0.84 mmol), aminoacetonitrile hydrochloride (155 mg, 1.68 mmol) in dry DMF (10 mL) under dry nitrogen was added triethylamine (0.38 mL, 2.67 mmol) dropwise and the reaction stirred for 2½ hours. Aqueous sat. NaHCO3 was added and the product extracted with Et2O (2×), dried over Na2SO4, concentrated in vacuo and purified by flash chromatography over silica gel (EtOAc/Hex, 4/6) to afford N1-(cyanomethyl)-N2-(4-{4-[4-(tert-butoxycarbonyl)piperazin-1-yl]phenyl}-1,2,5-oxadiazol-3-yl)leucinamide.
WORKUP
后处理
- extractionthe product extracted with Et2O (2×)
- dry with materialdried over Na2SO4
- concentrationconcentrated in vacuo
- custompurified by flash chromatography over silica gel (EtOAc/Hex, 4/6)