82752-99-6
82752-99-6 結(jié)構(gòu)式
基本信息
萘法唑酮鹽酸鹽
NEFAZODONE
BMY 13754-1
>=98% (HPLC)
Nefazodone HCl
NEFAZODONE-D5 HCL
Nefazodone hydrochlo
Nefazodone hydrochloride
Nefazodone hydrochloride API
Nefazodone Hydrochloride (200 mg)
1-(3-(4-(3-Chlorophenyl)piperazin-1-yl)propyl)-3-ethyl-4-(2-phenoxyethyl)-1H-1,2,4-triazol-5(4H)-
1-{3-[4-(3-chlorophenyl)piperazin-1-yl]propyl}-3-ethyl-4-(2-phenoxyethyl)-4,5-dihydro-1H-1,2,4-triazol-5-one
1-(3-(4-(3-Chlorophenyl)piperazin-1-yl)propyl)-3-ethyl-4-(2-phenoxyethyl)-1H-1,2,4-triazol-5(4H)-one hydrochloride
2,4-Dihydro-2-(3-(4-(3-chlorophenyl)-1-piperazinyl)propyl)-5-ethyl-4-(2-phenoxyethyl)-3H-1,2,4-triazol-3-one hydrochloride
3H-1,2,4-Triazol-3-one, 2-3-4-(3-chlorophenyl)-1-piperazinylpropyl-5-ethyl-2,4-dihydro-4-(2-phenoxyethyl)-, monohydrochloride
BMY-13754, MJ-13754-1, Serzone, 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl- 2,4-dihydro-4-(2-phenoxyethyl)-3H-1,2,4-triazol-3-one hydrochloride
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
常見問題列表
95885-13-5
52605-52-4
82752-99-6
實(shí)施例6：將5-乙基-4-(2-苯氧基乙基)-2H-1,2,4-三唑-3(4H)-酮（60.0 g，0.257 mol）、1-(3-氯苯基)-4-(3-氯丙基)哌嗪鹽酸鹽（79.7 g，0.257 mol）、氫氧化鈉（26.7 g，0.669 mol）和400 mL異丙醇混合，攪拌并加熱回流10至18小時(shí)。反應(yīng)完成后，用37%鹽酸（35 mL，0.42 mol）酸化反應(yīng)混合物，隨后減壓濃縮去除溶劑。將殘余物與400 mL二氯甲烷攪拌，過濾后減壓濃縮濾液。殘余物從600 mL異丙醇中結(jié)晶，得到81.5 g（62.5%收率）的2-[3-[4-(3-氯苯基)-1-哌嗪基]丙基]-5-乙基-2,4-二氫-4-(2-苯氧基乙基)-3H-1,2,4-三唑-3-酮鹽酸鹽。產(chǎn)物進(jìn)一步從水和異丙醇中結(jié)晶，得到純品，熔點(diǎn)為180°C-182.5°C。產(chǎn)物的光譜數(shù)據(jù)（NMR、13C NMR、IR）和元素分析結(jié)果與實(shí)施例2中獲得的相同產(chǎn)物數(shù)據(jù)一致。
參考文獻(xiàn)：
[1] Patent: US4487773, 1984, A
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5-HT 2A Receptor 5.8 nM (Ki) |
α1-adrenergic receptor
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Nefazodone hydrochloride (BMY-13754) is a phenylpiperazine antidepressant with a mechanism of action that is distinct from those of other currently available drugs. Nefazodone hydrochloride potently and selectively blocks postsynaptic serotonin (5-hydroxytryptamine; 5-HT) 5-HT2A receptors and moderately inhibits serotonin and noradrenaline (norepinephrine) reuptake. Nefazodone hydrochloride is also an inhibitor of the hepatic P-450 isoenzyme CYP3A4.