78818-15-2

基本信息
3-OXOPIPERAZINE-1-CARBOXYLIC ACID BENZYL ESTER
4-BENZYLOXYCARBONYL-2-PIPERAZINONE
4-BENZYLOXYCARBONYLPIPERAZIN-2-ONE
4-CBZ-PIPERAZINONE
4-Z-PIPERAZIN-2-ONE
BENZYL 3-OXOPIPERAZINE-1-CARBOXYLATE
BENZYL 3-OXOTETRAHYDRO-1(2H)-PYRAZINECARBOXYLATE
BUTTPARK 32\04-69
N'-Z-PIPERAZIN-2-ONE
Piperazin-2-one, N4-CBZ protected
1-CBZ-3-OXOPIPERAZINE
N-CBZ-PIPERAZINONE
N-CARBOXYBENZYLOXYPIPERAZINONE
3-Oxopiperazine-1-carboxylic acid benzyl ester, 4-Benzyloxycarbonyl-2-piperazinone
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
制備方法

5625-67-2

501-53-1

78818-15-2
步驟2: 3-氧代哌嗪-1-羧酸芐酯的合成 在0℃下,將碳酸鈉(24.77g,233.73mmol,3.00當(dāng)量)和哌嗪-2-酮(7.80g,77.91mmol,1.00當(dāng)量)溶于乙基乙酸酯(70.00mL)和水(70.00mL)的混合溶劑中。隨后,緩慢加入氯甲酸芐酯(16.79g,93.49mmol,13.99mL,純度95%,1.20當(dāng)量)。將反應(yīng)混合物在30℃下攪拌16小時(shí),通過TLC監(jiān)測反應(yīng)進(jìn)度。反應(yīng)完成后,用乙酸乙酯(80mL×3)萃取混合物。合并有機(jī)層,用飽和氯化鈉水溶液(80mL×3)洗滌,無水硫酸鈉干燥,減壓濃縮得到粗產(chǎn)物。粗產(chǎn)物通過打漿純化(石油醚:乙酸乙酯= 20:1,80mL),在30℃下攪拌15分鐘后過濾。固體經(jīng)真空干燥,得到4-芐氧羰基-2-哌嗪酮(15.50g,66.17mmol,收率84.93%),為白色固體。
參考文獻(xiàn):
[1] Journal of Organic Chemistry, 1991, vol. 56, # 11, p. 3715 - 3719
[2] Tetrahedron, 2010, vol. 66, # 18, p. 3370 - 3377
[3] Patent: EP3269715, 2018, A1. Location in patent: Paragraph 0238; 0239
[4] European Journal of Medicinal Chemistry, 2017, vol. 132, p. 26 - 41
[5] European Journal of Medicinal Chemistry, 1981, vol. 16, # 3, p. 229 - 232