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Piberaline fumarate, EGYT-475, Trelibet

1-苯甲基-4-(2-吡啶基羰基)哌拉嗪(E)-2-丁烯二酸盐(1:1)吡贝拉林Chemical Name: 1-Phenylmethyl-4-(2-pyridylcarbonyl)piperazine (E)-2-butenedioate (1:1); 1-Benzyl-4-picolinoylpiperazine fumarate (1:1)
CAS No. 39640-14-7, 39640-12-5 (diHCl), 39640-15-8 (free base)
项目整合开发状态: Phase II
项目研究机构: Egis (Originator)
合成路线:This compound can be obtained in three different ways:1) Condensation of pyridine-2-carboxylic acid (Ia,R = H),with 1-phenyl methylpiperazine (II) at 160 C.2) Condensation of methyl pyridine-2-carboxylate (Ib,R = CH3) with 1-phenylmethylpiperazine (II) at 140 C.3) Reaction of 1-phenylmethylpiperazine (II) with a mixed anhydride (III) formed from (Ia) and ethyl chloroformate (IV).
📌 参考资料/链接:
参考文献标题:Preparation of pyridinecaboxylic acid piperazides
文献作者:Budai,Z.; Mezei,T.; Lay,A.(Egis Pharmaceuticals Ltd.)
参考来源:DE 2828888; GB 2001062; HU 175075

📄 详细内容


合成路线:This compound can be obtained in three different ways:1) Condensation of pyridine-2-carboxylic acid (Ia,R = H),with 1-phenyl methylpiperazine (II) at 160 C.2) Condensation of methyl pyridine-2-carboxylate (Ib,R = CH3) with 1-phenylmethylpiperazine (II) at 140 C.3) Reaction of 1-phenylmethylpiperazine (II) with a mixed anhydride (III) formed from (Ia) and ethyl chloroformate (IV).

参考文献标题:Pyridine derivatives
文献作者:Ki,J.; et al.(Egis Pharmaceuticals Ltd.)
参考来源:DE 2215545; GB 1378964; HU 162396; JP 7644957


合成路线:This compound can be obtained in three different ways:1) Condensation of pyridine-2-carboxylic acid (Ia,R = H),with 1-phenyl methylpiperazine (II) at 160 C.2) Condensation of methyl pyridine-2-carboxylate (Ib,R = CH3) with 1-phenylmethylpiperazine (II) at 140 C.3) Reaction of 1-phenylmethylpiperazine (II) with a mixed anhydride (III) formed from (Ia) and ethyl chloroformate (IV).

参考文献标题:Piberaline
文献作者:N骻r醖i,M.
参考来源:Drugs Fut 1984,9(1),30


合成路线:This compound can be obtained in three different ways:1) Condensation of pyridine-2-carboxylic acid (Ia,R = H),with 1-phenyl methylpiperazine (II) at 160 C.2) Condensation of methyl pyridine-2-carboxylate (Ib,R = CH3) with 1-phenylmethylpiperazine (II) at 140 C.3) Reaction of 1-phenylmethylpiperazine (II) with a mixed anhydride (III) formed from (Ia) and ethyl chloroformate (IV).

参考文献标题:Synthesis of 14C and 3H specifically labelled 1-benzyl-4-picolinoylpiperazine
文献作者:Budai,Z.; Z髄yomi,G.
参考来源:J Label Compd Radiopharm 1981,18427-432


合成路线:This compound can be obtained in three different ways:1) Condensation of pyridine-2-carboxylic acid (Ia,R = H),with 1-phenyl methylpiperazine (II) at 160 C.2) Condensation of methyl pyridine-2-carboxylate (Ib,R = CH3) with 1-phenylmethylpiperazine (II) at 140 C.3) Reaction of 1-phenylmethylpiperazine (II) with a mixed anhydride (III) formed from (Ia) and ethyl chloroformate (IV).
参考文献标题:A novel synthesis of pyridinecarboxylic acid piperazides
文献作者:Budai,Z.; Mezei,T.; Lay,A.
参考来源:Acta Chim Acad Sci Hung 1980,105241-246


产品链接: CAS No. 39640-14-7››

产品链接: CAS No.39640-15-8››