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Taltirelin, TA-0910, Ceredist

他替瑞林Chemical Name: (S)-1-Methyl-4,5-dihydroorotyl-L-histidyl-L-prolinamide; (S)-N-(1-Methyl-2,6-dioxohexahydropyrimidin-4-ylcarbonyl)-L-histidyl-L-prolinamide
CAS No. 103300-74-9
项目整合开发状态: Launched-2000
项目研究机构: Tanabe Seiyaku (Orphan Drug), Tanabe Seiyaku (Originator)
合成路线:The methylation of 4,5-dihydroorotic acid benzyl ester (I) with methyl iodide gives the corresponding 1-methyl derivative (II),which is debenzylated by hydrogenolysis with H2 over Pd/C yielding (S)-1-methyl-4,5-dihydroorotic acid (III).Finally,this compound is condensed with L-histidyl-L-prolinamide (IV) by means of dicyclohexylcarbodiimide (DCC) and N-hydroxysuccinimide (HONSU) in DMF.
📌 参考资料/链接:
参考文献标题:Dihydroorotic acid derivs.,process for their preparing and pharmaceutical compsn.containing them
文献作者:Sugano,H.; Ishida,R.; Yamamura,M.(Tanabe Seiyaku Co.,Ltd.)
参考来源:EP 0168042; ES 8705463; ES 8707738; ES 8800208; US 4665056

📄 详细内容


合成路线:The methylation of 4,5-dihydroorotic acid benzyl ester (I) with methyl iodide gives the corresponding 1-methyl derivative (II),which is debenzylated by hydrogenolysis with H2 over Pd/C yielding (S)-1-methyl-4,5-dihydroorotic acid (III).Finally,this compound is condensed with L-histidyl-L-prolinamide (IV) by means of dicyclohexylcarbodiimide (DCC) and N-hydroxysuccinimide (HONSU) in DMF.

参考文献标题:Dihydroorotic acid derivs.and process for their preparation
文献作者:Sugano,H.; Ishida,R.; Yamamura,M.(Tanabe Seiyaku Co.,Ltd.)
参考来源:JP 1986033197


合成路线:The methylation of 4,5-dihydroorotic acid benzyl ester (I) with methyl iodide gives the corresponding 1-methyl derivative (II),which is debenzylated by hydrogenolysis with H2 over Pd/C yielding (S)-1-methyl-4,5-dihydroorotic acid (III).Finally,this compound is condensed with L-histidyl-L-prolinamide (IV) by means of dicyclohexylcarbodiimide (DCC) and N-hydroxysuccinimide (HONSU) in DMF.

参考文献标题:Therapeutic agent for central nervous system disorders
文献作者:Sugano,H.; Ishida,R.; Yamamura,M.(Tanabe Seiyaku Co.,Ltd.)
参考来源:JP 1987234029


合成路线:The methylation of 4,5-dihydroorotic acid benzyl ester (I) with methyl iodide gives the corresponding 1-methyl derivative (II),which is debenzylated by hydrogenolysis with H2 over Pd/C yielding (S)-1-methyl-4,5-dihydroorotic acid (III).Finally,this compound is condensed with L-histidyl-L-prolinamide (IV) by means of dicyclohexylcarbodiimide (DCC) and N-hydroxysuccinimide (HONSU) in DMF.

参考文献标题:Synthesis and central nervous system actions of thyrotropin-releasing hormone analogues containing a dihydroorotic acid moiety
文献作者:Suzuki,M.; Sugano,H.; Matsumoto,K.; Yamamura,M.; Ishida,R.
参考来源:J Med Chem 1990,33(8),2130-37


合成路线:The methylation of 4,5-dihydroorotic acid benzyl ester (I) with methyl iodide gives the corresponding 1-methyl derivative (II),which is debenzylated by hydrogenolysis with H2 over Pd/C yielding (S)-1-methyl-4,5-dihydroorotic acid (III).Finally,this compound is condensed with L-histidyl-L-prolinamide (IV) by means of dicyclohexylcarbodiimide (DCC) and N-hydroxysuccinimide (HONSU) in DMF.
参考文献标题:TA-0910
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1991,16(2),127


产品链接: CAS No. 103300-74-9››