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【结 构 式】

【药物名称】Lomerizine hydrochloride, DE-090, KB-2796, Terranas, Migsis

【化学名称】1-[Bis(4-fluorophenyl)methyl]-4-(2,3,4-trimethoxy-benzyl)piperazine dihydrochloride

【CA登记号】101477-54-7, 101477-55-8 (free base)

【 分 子 式 】C27H32Cl2F2N2O3

【 分 子 量 】541.47049

【开发单位】Nippon Organon (Originator), Pfizer (Licensee), Santen (Licensee)

【药理作用】ANALGESIC AND ANESTHETIC DRUGS, Antiglaucoma Agents, Antimigraine Drugs, Migraine, Prophylactic Treatment of, OCULAR MEDICATIONS, Ophthalmic Drugs, Calcium Channel Blockers, P-Glycoprotein (MDR-1) Inhibitors

合成路线1

By reductocondensation of 2,3,4-trimethoxybenzaldehyde (I) with l-[bis(4-fluorophenyl)methyl] piperazine (II) by means of formic acid at 100-120 C.

1 Stukamoto, G.; Kanazawa, T.; Ohtaka, H.; Ito, K.; Benzylpiperazine derivatives. IV. Synthesis and ce. Chem Pharm Bull 1987, 35, 8, 3270.
2 Ito, K.; Kanazawa, T.; Ohtaka, H.; Tsukamoto, G. (Kanebo Pharmaceuticals, Ltd.); 1-(2,3,4-Tri-methoxybenzyl)-4[bis(4-fluorophenyl)m. EP 0159566; ES 8702393; ES 8801236; ES 8801237; JP 1985222472; US 4663325 .
3 Prous, J.; Castaner, J.; KB-2796. Drugs Fut 1988, 13, 4, 312.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 16838 1-Bis(4-fluorophenyl)methyl piperazine; 1-[bis(4-fluorophenyl)methyl]piperazine 27469-60-9 C17H18F2N2 详情 详情
(II) 22119 2,3,4-trimethoxybenzaldehyde 2103-57-3 C10H12O4 详情 详情
Extended Information