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Meldonium hydrate, Quaterin, Mildronate, MET-88, Q-4224-IOS,

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摘 要:Meldonium hydrate, Quaterin, Mildronate, MET-88, Q-4224-IOS, THP(anhydrous),86426-17-7, 76144-81-5 (anhydrous),C6-H14-N2-O2.2-H2-O,3-(2,2,2-Trimethylhydrazinium)propionate dihydrate; 2-(2-Carboxyethyl)-1,1,1-trimethylhydrazinium hydroxyde inner salt
  • 【药物名称】Meldonium hydrate, Quaterin, Mildronate, MET-88, Q-4224-IOS, THP(anhydrous)
  • 【化学名】3-(2,2,2-Trimethylhydrazinium)propionate dihydrate; 2-(2-Carboxyethyl)-1,1,1-trimethylhydrazinium hydroxyde inner salt dihydrate
  • 【CAS登记号】86426-17-7, 76144-81-5 (anhydrous)
  • 【结构式】Meldonium hydrate, Quaterin, Mildronate, MET-88, Q-4224-IOS,--药物合成数据库
  • 【分子式】C6-H14-N2-O2.2-H2-O
  • 【分子量】182.2182
  • 【原研厂家】Latvian Institute of Organic Synthesis (Originator), Taiho (Licensee)
  • 【作用类别】Acute Myocardial Infarction, Treatment of, Angina pectoris, Treatment of, CARDIOVASCULAR DRUGS, Treatment of Disorders of the Coronary Arteries and Atherosclerosis
  • 【研发状态】Phase II
  • 【合成情况】 
  • 〖来源〗Drugs Fut
  • 〖合成路线〗
  • 〖标题〗MILDRONATE
  • 〖合成方法〗Methyl 3-(2,2-dimethylhydrazino)propionate (I) is treated with a methyl halide (II, X = halo) or dimethyl sulfate (II, X = CH3SO4) to give the appropriate trimethylhydrazinium salt (III), which is transferred to 3-(2,2,2-trimethylhydrazinium)propionate (IV) by Amberlite IRA-400 (OH form). After crystallization from ethanol the inner salt is obtained as a dihydrate.
  • 〖作者〗Prous, J.; Castaer, J.
  • 〖参考〗Prous, J.; Castaer, J.; MILDRONATE. Drugs Fut 1989, 14, 1, 29
  • 〖出处〗Drugs Fut1989,14,(1):29
  • 〖备注〗Methyl 3-(2,2-dimethylhydrazino)propionate (I) is treated with a methyl halide (II, X=halo) or dimethyl sulfate (II, X=CH3SO4) to give the appropriate trimethylhydrazinium salt (III) which is transferred to 3-(2,2,2-trimethylhydrazinium)propionate (IV) by Amberlite IRA-400 (OH form). After crystallization from ethanol the inner salt is obtained as a dihydrate (1-5). Description Colorless crystals, slightly hygroscopic, m.p. 254-6?(1-5). Source Inst. Org. Synth., Latvian SSR Acad. Sci., Riga (USSR). References 1. Goldberg, Yu.Sh., Abele, E., Kalvinsh, I.Ya., Bremanis, G., Shimanskaya, M.V. and Lukevicz, E.Ya. Dokl Akad Nauk SSSR (Khim) 1987, 294: 1387. 2. Kemme, A., Bleidelis, J., Kalvinsh, I.Ya. and Eremeeva, A.V. Latv PSR Zinat Akad Vestis 1983, 2: 215. 3. Kalvinsh, I.Ya., Vinogradov, A.V., Veveris, M., Makarova, I.I., Birman, A.S., Barmotin, G.V., Akifiev, O.N. (Inst. Org. Synth., Acad. Sci. Latv. SSR) and Pirogov, N.I. (Moscow State Med. Inst.) DE 3234537. 4. Giller, S.A., Eremeev, A.V., Kalvinsh, I.Ya., Semenikhina, V.G., Liepinsh, E.A., Anderson, P.P., Astapenok, E.B., Sprunzh, Y.Y., Trapetsiers, P.T. and Podprigora, G.I. (Inst. Org. Synth., Acad. Sci. Latv. SSR) WO 8001068. 5. Eremeev, A.V., Kalvinsh, I.Ya., Semenkhina, V.G., Liepinsh, E.A., Latvietis, J., Anderson, P.P., Astapenok, E.B., Spruzh, Y.Y and Trapetsiers, P.T. (Inst. Org. Synth., Acad. Sci. Latv. SSR) FR 2478087.
  • 〖来源〗Latv Psr Zinat Akad Vestis
  • 〖合成路线〗
  • 〖标题〗Molecular-crystalline structure of 3-(2,2, 2-trimethylhydrazinio)propionate dihydrate C6H14N2O2.2H2O
  • 〖合成方法〗Methyl 3-(2,2-dimethylhydrazino)propionate (I) is treated with a methyl halide (II, X = halo) or dimethyl sulfate (II, X = CH3SO4) to give the appropriate trimethylhydrazinium salt (III), which is transferred to 3-(2,2,2-trimethylhydrazinium)propionate (IV) by Amberlite IRA-400 (OH form). After crystallization from ethanol the inner salt is obtained as a dihydrate.
  • 〖作者〗Kemme, A.; Bleidelis, J.; Kalvins, I.; Eremeev, A.V.
  • 〖参考〗Kemme, A.; Bleidelis, J.; Kalvins, I.; Eremeev, A.V.; Molecular-crystalline structure of 3-(2,2, 2-trimethylhydrazinio)propionate dihydrate C6H14N2O2.2H2O. Latv Psr Zinat Akad Vestis 1983, 2, 215-8
  • 〖出处〗Latv Psr Zinat Akad Vestis1983,2,():215-8
  • 〖备注〗
  • 〖来源〗Dokl Akad Nauk SSSR (Khim)
  • 〖合成路线〗
  • 〖标题〗
  • 〖合成方法〗Methyl 3-(2,2-dimethylhydrazino)propionate (I) is treated with a methyl halide (II, X = halo) or dimethyl sulfate (II, X = CH3SO4) to give the appropriate trimethylhydrazinium salt (III), which is transferred to 3-(2,2,2-trimethylhydrazinium)propionate (IV) by Amberlite IRA-400 (OH form). After crystallization from ethanol the inner salt is obtained as a dihydrate.
  • 〖作者〗Bremanis, G.; Shimanskaya, M.V.; Lukevicz, E.Ya.; Kalvinsh, I.Ya.; Goldberg, Yu. Sh.; Abele, E.
  • 〖参考〗Bremanis, G.; Shimanskaya, M.V.; Lukevicz, E.Ya.; Kalvinsh, I.Ya.; Goldberg, Yu. Sh.; Abele, E.; . Dokl Akad Nauk SSSR (Khim) 1987, 294, 1387
  • 〖出处〗Dokl Akad Nauk SSSR (Khim)1987,294,():1387
  • 〖备注〗
  • 〖来源〗WO 8001068
  • 〖合成路线〗
  • 〖标题〗3-(2,2,2-Trimethylhydrazinium)propionate, method of obtaining it and use
  • 〖合成方法〗Methyl 3-(2,2-dimethylhydrazino)propionate (I) is treated with a methyl halide (II, X = halo) or dimethyl sulfate (II, X = CH3SO4) to give the appropriate trimethylhydrazinium salt (III), which is transferred to 3-(2,2,2-trimethylhydrazinium)propionate (IV) by Amberlite IRA-400 (OH form). After crystallization from ethanol the inner salt is obtained as a dihydrate.
  • 〖作者〗Guiller, S.A.; Eremeev, A.V.; Kalvinsh, I.Y.; Semenikhina, V.G.; Liepinsh, E.A.; Latvietis, Y.Y.; Anderson, P.P.; Astapenok, E.B.; Spruzh, Y.Y.; Trapetsiers, P.T.; Podoprigora, G.I. (Latvian Institute of Organic Synthesis)
  • 〖参考〗Guiller, S.A.; Eremeev, A.V.; Kalvinsh, I.Y.; Semenikhina, V.G.; Liepinsh, E.A.; Latvietis, Y.Y.; Anderson, P.P.; Astapenok, E.B.; Spruzh, Y.Y.; Trapetsiers, P.T.; Podoprigora, G.I. (Latvian Institute of Organic Synthesis); 3-(2,2,2-Trimethylhydrazinium)p55273-05-7 (free base)/li> li>??p耀?ul class="old_
  • 〖出处〗WO 8001068,,():
  • 〖备注〗
  • 〖来源〗FR 2478087
  • 〖合成路线〗
  • 〖标题〗3-(2,2,2-Trimethylhydrazinium)propionate, process for their preparation and use
  • 〖合成方法〗Methyl 3-(2,2-dimethylhydrazino)propionate (I) is treated with a methyl halide (II, X = halo) or dimethyl sulfate (II, X = CH3SO4) to give the appropriate trimethylhydrazinium salt (III), which is transferred to 3-(2,2,2-trimethylhydrazinium)propionate (IV) by Amberlite IRA-400 (OH form). After crystallization from ethanol the inner salt is obtained as a dihydrate.
  • 〖作者〗Eremeev, A.V.; Kalvinsh, V.G.; Semenikhina, V.G.; Liepinsh, E.E.; Latvietis, Y.Y.; Anderson, P.P.; Astapenok, F.B.; Spuzh, Y.Y.; Trapentsiers, G.T.; Podoprigora, G.I.; Giller, S.A. (Latvian Institute of Organic Synthesis)
  • 〖参考〗Eremeev, A.V.; Kalvinsh, V.G.; Semenikhina, V.G.; Liepinsh, E.E.; Latvietis, Y.Y.; Anderson, P.P.; Astapenok, F.B.; Spuzh, Y.Y.; Trapentsiers, G.T.; Podoprigora, G.I.; Giller, S.A. (Latvian Institute of Organic Synthesis); 3-(2,2,2-Trimethylhydrazinium)pr55273-05-7 (free base)/li> li>??p耀?ul class="old_db">l
  • 〖出处〗FR 2478087,,():
  • 〖备注〗
  • 〖来源〗DE 3234537; GB 2105992; JP 58074606; US 4451485
  • 〖合成路线〗
  • 〖标题〗Treatment of cardiovascular diseases with 3-(2,2,2-trimethylhydrazinium) propionate dihydrate.
  • 〖合成方法〗Methyl 3-(2,2-dimethylhydrazino)propionate (I) is treated with a methyl halide (II, X = halo) or dimethyl sulfate (II, X = CH3SO4) to give the appropriate trimethylhydrazinium salt (III), which is transferred to 3-(2,2,2-trimethylhydrazinium)propionate (IV) by Amberlite IRA-400 (OH form). After crystallization from ethanol the inner salt is obtained as a dihydrate.
  • 〖作者〗Kalvinsh, I.Y.; Vinogradov, A.V.; Veveris, M.M.; Makarova, I.I.; Birman, A.S.; Barmotin, G.V.; Akifiev, O.N. (Institu Orch Sinteza Akademii)
  • 〖参考〗Kalvinsh, I.Y.; Vinogradov, A.V.; Veveris, M.M.; Makarova, I.I.; Birman, A.S.; Barmotin, G.V.; Akifiev, O.N. (Institu Orch Sinteza Akademii); Treatment of cardiovascular diseases with 3-(2,2,2-trimethylhydrazinium) propionate dihydrate.. DE 3234537; GB 2155273-05-7 (free base)/li> l
  • 〖出处〗DE 3234537; GB 2105992; JP 58074606; US 4451485,,():
  • 〖备注〗
 
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