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CAS 289686-69-7

2-(3,5-bis(trifluoromethyl)phenyl)-2-methylpropanoyl chloride2-[3,5-Bis(trifluoromethyl)phenyl]-2-methylpropanoyl chloride

登记编号:Elinzanetant-012、(IX)448314-1-a、(XIX)448314-2-b、FOSNE-011、NETUP-010

应用背景(按来源药适应症)

热潮红依林奈坦血管舒缩症依林奈坦HR阳性乳腺癌依林奈坦睡眠障碍依林奈坦绝经期症状依林奈坦阿片类依赖依林奈坦化疗导致的恶心和呕吐福奈妥匹坦化疗导致的恶心和呕吐奈妥吡坦肿瘤奈妥吡坦

来源药(使用该中间体的合成路线)

品种梯队到期年
依林奈坦ElinzanetantTier C · 观察 / 贸易-
福奈妥匹坦FosnetupitantTier C · 观察 / 贸易-
奈妥吡坦NetupitantTier C · 观察 / 贸易-

合成路线中的位置(上下游链)

按路线登记顺序排列,左→右为合成方向;高亮为当前 CAS,其余可点击跳转对应档案。

依林奈坦优化路线步数:8总收率:/
3-Amino-6-chloropyridine→1,1-Dimethylethyl (6-Chloro-3-pyridinyl)carbamate→N-(6-Chloro-4-iodopyridin-3-yl)carbamic acid tert-butyl ester→Iodomethane→6-Chloro-4-iodo-N-methyl-N-Boc-pyridin-3-amine→6-Chloro-4-iodo-N-methylpyridin-3-amine→4-Fluoro-2-methylphenylboronic acid→6-Chloro-4-(4-fluoro-2-methylphenyl)-N-methylpyridin-3-amine→2-[3,5-Bis(trifluoromethyl)phenyl]-2-methylpropanoyl chloride→2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-N,2-dimethylpropanamide→(7S,9aS)-7-([[tert-Butyl(dimethyl)silyl]oxy]methyl)octahydropyrazino[2,1-c][1,4]oxazine→2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-[(7S,9aS)-7-([[tert-butyl(dimethyl)silyl]oxy]methyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-N,2-dimethylpropanamide
依林奈坦优化路线步数:5总收率:/
2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-N,2-dimethylpropanamide→4-Chloro-5-nitropyridin-2(1H)-one→2-[3,5-Bis(trifluoromethyl)phenyl]-2-methylpropanoyl chloride→4-Fluoro-2-methylphenylboronic acid→4-(4-Fluoro-2-methylphenyl)-5-nitropyridin-2(1H)-one→2-Chloro-4-(4-fluoro-2-methylphenyl)-5-nitropyridine→6-Chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-amine hydrogen chloride (1/1)→2-[3,5-Bis(trifluoromethyl)phenyl]-2-methylpropanoic acid→2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-2-methylpropanamide→Iodomethane

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Unibest Nantong cGMP Site2-(3,5-bis-trifluoromethylphenyl)-2-methyl-propionyl chloride
Pharmaceutical Intermediates
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