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Tomoxiprole, MDL-035,76145-76-1,C21-H20-N2-O,3-Isopropyl-2-(

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摘 要:Tomoxiprole, MDL-035,76145-76-1,C21-H20-N2-O,3-Isopropyl-2-(4-methoxyphenyl)-3H-naphth[1,2-d]imidazole
  • 【药物名称】Tomoxiprole, MDL-035
  • 【化学名】3-Isopropyl-2-(4-methoxyphenyl)-3H-naphth[1,2-d]imidazole
  • 【CAS登记号】76145-76-1
  • 【结构式】Tomoxiprole, MDL-035,76145-76-1,C21-H20-N2-O,3-Isopropyl-2-(--药物合成数据库
  • 【分子式】C21-H20-N2-O
  • 【分子量】316.402
  • 【原研厂家】Lepetit (Originator)
  • 【作用类别】ANALGESIC AND ANESTHETIC DRUGS, Analgesic Drugs, Non-Opioid Analgesics, Non-Steroidal Antiinflammatory Drugs
  • 【研发状态】Preclinical
  • 【合成情况】 
  • 〖来源〗Drugs Fut
  • 〖合成路线〗
  • 〖标题〗Tomoxiprole
  • 〖合成方法〗Reaction of 1-nitroso-2-naphthol (I) with isopropylamine in water gives 2-isopropylamino-1-nitrosonaphthalene (II). After hydrogenation, condensation of the resulting 2-isopropylamino-1,2-naphthalendiamine (III) with p-methoxybenzaldehyde yields the 1,2-dihydro derivative (IV), which is converted to MDL-035 with palladium on carbon. Toluene is used as a solvent throughout the synthesis. The overall yield on a 20-kg scale is 57%.
  • 〖作者〗Castaer, J.; Chu, S.S.; Serradell, M.N.
  • 〖参考〗Castaer, J.; Chu, S.S.; Serradell, M.N.; Tomoxiprole. Drugs Fut 1985, 10, 2, 133
  • 〖出处〗Drugs Fut1985,10,(2):133
  • 〖备注〗Synthesis of 090565: Reaction of 1-nitroso-2-naphthol (I) with isopropylamine in water gives 2-isopropylamino-1-nitrosonaphthalene (II). After hydrogenation, condensation of the resulting 2-isopropylamino-1,2-naphthalendiamine (III) with p-methoxy benzaldehyde yields the 1,2-dihydro derivative (IV), which is converted to MDL-035 with palladium on carbon. Toluene is used as a solvent throughout the synthesis. The overall yield on a 20-kg scale is 57% (1,2). (Scheme 09056501a) Description White, odorless, tasteless crystalline powder, m.p. 160-1? practically insoluble in pure water and alkaline aqueous solutions, but slightly soluble in simulated gastric juice (pH<2). All pharmacological and toxicological tests were done with the micronized form. Particle size distribution <20 microm., 90% in volume. Manufacturer Gruppo Lepetit SpA, Milan (Italy) References 1. Toja, E., Selva, D. and Schiatti, P.; 3-Alkyl-2-aryl-3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflamatory agents.; J Med Chem 1984, 27; 610-616 2. Toja, E., Omodei-Sal? A. and Selva, D. (Grupo Lepetit SpA); EP 12.866, JP 80.92.376, US 4.340.607, US 4.435.417
  • 〖来源〗J Med Chem
  • 〖合成路线〗
  • 〖标题〗3-Alkyl-2-ary?3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflammatory agents
  • 〖合成方法〗Reaction of 1-nitroso-2-naphthol (I) with isopropylamine in water gives 2-isopropylamino-1-nitrosonaphthalene (II). After hydrogenation, condensation of the resulting 2-isopropylamino-1,2-naphthalendiamine (III) with p-methoxybenzaldehyde yields the 1,2-dihydro derivative (IV), which is converted to MDL-035 with palladium on carbon. Toluene is used as a solvent throughout the synthesis. The overall yield on a 20-kg scale is 57%.
  • 〖作者〗Toja, E.; Schiatti, P.; Selva, D.
  • 〖参考〗Toja, E.; Schiatti, P.; Selva, D.; 3-Alkyl-2-ary?3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflammatory agents. J Med Chem 1984, 27, 5, 610-616
  • 〖出处〗J Med Chem1984,27,(5):610-616
  • 〖备注〗Synthesis of 090565: Reaction of 1-nitroso-2-naphthol (I) with isopropylamine in water gives 2-isopropylamino-1-nitrosonaphthalene (II). After hydrogenation, condensation of the resulting 2-isopropylamino-1,2-naphthalendiamine (III) with p-methoxy benzaldehyde yields the 1,2-dihydro derivative (IV), which is converted to MDL-035 with palladium on carbon. Toluene is used as a solvent throughout the synthesis. The overall yield on a 20-kg scale is 57%. (Scheme 09056501a) Description White, odorless, tasteless crystalline powder, m.p. 160-1? practically insoluble in pure water and alkaline aqueous solutions, but slightly soluble in simulated gastric juice (pH<2). All pharmacological and toxicological tests were done with the micronized form. Particle size distribution <20 microm., 90% in volume.
  • 〖来源〗EP 0012866; JP 8092376; US 4340607; US 4435417
  • 〖合成路线〗
  • 〖标题〗Antimicrobial 3H-naphto[1,2-d]imidazoles
  • 〖合成方法〗Reaction of 1-nitroso-2-naphthol (I) with isopropylamine in water gives 2-isopropylamino-1-nitrosonaphthalene (II). After hydrogenation, condensation of the resulting 2-isopropylamino-1,2-naphthalendiamine (III) with p-methoxybenzaldehyde yields the 1,2-dihydro derivative (IV), which is converted to MDL-035 with palladium on carbon. Toluene is used as a solvent throughout the synthesis. The overall yield on a 20-kg scale is 57%.
  • 〖作者〗Toja, E.; Omodei-Sale, A.; Selva, D. (Lepetit SpA)
  • 〖参考〗Toja, E.; Omodei-Sale, A.; Selva, D. (Lepetit SpA); Antimicrobial 3H-naphto[1,2-d]imidazoles. EP 0012866; JP 8092376; US 4340607; US 4435417
  • 〖出处〗EP 0012866; JP 8092376; US 4340607; US 4435417,,():
  • 〖备注〗Synthesis of 090565: Reaction of 1-nitroso-2-naphthol (I) with isopropylamine in water gives 2-isopropylamino-1-nitrosonaphthalene (II). After hydrogenation, condensation of the resulting 2-isopropylamino-1,2-naphthalendiamine (III) with p-methoxy benzaldehyde yields the 1,2-dihydro derivative (IV), which is converted to MDL-035 with palladium on carbon. Toluene is used as a solvent throughout the synthesis. The overall yield on a 20-kg scale is 57%. (Scheme 09056501a) Description White, odorless, tasteless crystalline powder, m.p. 160-1? practically insoluble in pure water and alkaline aqueous solutions, but slightly soluble in simulated gastric juice (pH<2). All pharmacological and toxicological tests were done with the micronized form. Particle size distribution <20 microm., 90% in volume.
 
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