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BGP-15,66611-37-8 (tautomer),C14-H22-N4-O2.2-Cl-H,N'-[2-Hydr

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摘 要:BGP-15,66611-37-8 (tautomer),C14-H22-N4-O2.2-Cl-H,N'-[2-Hydroxy-3-(1-piperidinyl)propoxy]pyridine-3-carboxamidine dihydrochloride
  • 【药物名称】BGP-15
  • 【化学名】N'-[2-Hydroxy-3-(1-piperidinyl)propoxy]pyridine-3-carboxamidine dihydrochloride
  • 【CAS登记号】66611-37-8 (tautomer)
  • 【结构式】BGP-15,66611-37-8 (tautomer),C14-H22-N4-O2.2-Cl-H,N'-[2-Hydr--药物合成数据库
  • 【分子式】C14-H22-N4-O2.2-Cl-H
  • 【分子量】351.2756
  • 【原研厂家】N-Gene (Originator), Allos (Licensee), Chinoin (Licensee)
  • 【作用类别】Acute Myocardial Infarction, Treatment of, CARDIOVASCULAR DRUGS, Chemoprotective Agents, ONCOLYTIC DRUGS, Radioprotectants, Treatment of Disorders of the Coronary Arteries and Atherosclerosis, NAD+ ADP-Ribosyltransferase (poly(ADP-ribose)polymerase; PARP) Inhibitors
  • 【研发状态】Discontinued
  • 【合成情况】 
  • 〖来源〗WO 9008131
  • 〖合成路线〗
  • 〖标题〗Improved process for the preparation of amidoxime derivs.
  • 〖合成方法〗N-(2,3-Epoxypropyl)piperidine (III), prepared from piperidine (I) and epichlorhydrin (II), was condensed with nicotinic acid amidoxime (IV) in the presence of basic catalysts, such as NaOH, t-BuOK, Al2O3 or SnO2, in hot DMF to provide the title compound, which was finally converted to the dihydrochloride salt.
  • 〖作者〗Somfai, ?; Bertk, B.; Szkely, I.; Takcs, K.; Thurner, A.; Gajry, A.; Botr, S.; Nagy, L. (Chinoin Pharmaceutical and Chemical Works Co., Ltd.)
  • 〖参考〗Somfai, ?; Bertk, B.; Szkely, I.; Takcs, K.; Thurner, A.; Gajry, A.; Botr, S.; Nagy, L. (Chinoin Pharmaceutical and Chemical Works Co., Ltd.); Improved process for the preparation of amidoxime derivs.. WO 9008131
  • 〖出处〗WO 9008131,,():
  • 〖备注〗Synthesis of 278220: N-(2,3-Epoxypropyl)piperidine (III), prepared from piperidine (I) and epichlorhydrin (II), was condensed with nicotinic acid amidoxime (IV) in the presence of basic catalysts, such as NaOH, KOtBu, Al2O3 or SnO2, in hot DMF to provide the title compound, that was finally converted to the dihydrochloride salt. (Scheme 27822001a) Alternatively, the title compound was prepared by condensation of nicotinamidoxime (IV) with 1,1-pentamethylene-3-hdroxyazetidinium chloride (V). (Scheme 27822002a)
  • 〖来源〗WO 9008131
  • 〖合成路线〗
  • 〖标题〗Improved process for the preparation of amidoxime derivs.
  • 〖合成方法〗Alternatively, the title compound was prepared by condensation of nicotinamidoxime (IV) with 1,1-pentamethylene-3-hdroxyazetidinium chloride (V).
  • 〖作者〗Somfai, ?; Bertk, B.; Szkely, I.; Takcs, K.; Thurner, A.; Gajry, A.; Botr, S.; Nagy, L. (Chinoin Pharmaceutical and Chemical Works Co., Ltd.)
  • 〖参考〗Somfai, ?; Bertk, B.; Szkely, I.; Takcs, K.; Thurner, A.; Gajry, A.; Botr, S.; Nagy, L. (Chinoin Pharmaceutical and Chemical Works Co., Ltd.); Improved process for the preparation of amidoxime derivs.. WO 9008131
  • 〖出处〗WO 9008131,,():
  • 〖备注〗Synthesis of 278220: N-(2,3-Epoxypropyl)piperidine (III), prepared from piperidine (I) and epichlorhydrin (II), was condensed with nicotinic acid amidoxime (IV) in the presence of basic catalysts, such as NaOH, KOtBu, Al2O3 or SnO2, in hot DMF to provide the title compound, that was finally converted to the dihydrochloride salt. (Scheme 27822001a) Alternatively, the title compound was prepared by condensation of nicotinamidoxime (IV) with 1,1-pentamethylene-3-hdroxyazetidinium chloride (V). (Scheme 27822002a)
  • 〖来源〗US 4308399
  • 〖合成路线〗
  • 〖标题〗O-(3-Amino-2-hydroxy-propyl)amidoxime derivs., process for the preparation thereof and pharmaceutical compsns. containing same
  • 〖合成方法〗In a further procedure, nicotinamidoxime (IV) was condensed with 1-chloro-3-piperidino-2-propanol (VI) in the presence of ethanolic NaOEt.
  • 〖作者〗Farago, K.; Literati, P.N.; Simay, A.; Takacs, K.; Virag, S.; Szcntivanyi, M.; Kiss, I. (Chinoin Pharmaceutical and Chemical Works Co., Ltd.)
  • 〖参考〗Farago, K.; Literati, P.N.; Simay, A.; Takacs, K.; Virag, S.; Szcntivanyi, M.; Kiss, I. (Chinoin Pharmaceutical and Chemical Works Co., Ltd.); O-(3-Amino-2-hydroxy-propyl)amidoxime derivs., process for the preparation thereof and pharmaceutical compsns. cww.chemdrug.com/extend/view
  • 〖出处〗US 4308399,,():
  • 〖备注〗
 
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