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CAS 77-78-1

Dimethoxysulfone

登记编号:(XXXIII)638294-1-d、(XXII)1225102-2-b、(XIV)1157260-2-b

应用背景(按来源药适应症)

收缩性心力衰竭非奈利酮舒张期心力衰竭非奈利酮心脏衰竭非奈利酮慢性肾功能不全非奈利酮糖尿病肾病非奈利酮二型糖尿病非奈利酮非小细胞肺癌氟泽雷塞结直肠癌氟泽雷塞实体瘤氟泽雷塞非小细胞肺癌宗艾替尼肺癌宗艾替尼食道腺癌宗艾替尼食管胃结合部肿瘤宗艾替尼胃癌宗艾替尼转移性乳腺癌宗艾替尼

来源药(使用该中间体的合成路线)

品种梯队到期年
非奈利酮FinerenoneTier C · 观察 / 贸易2030
氟泽雷塞FulzerasibTier C · 观察 / 贸易-
宗艾替尼ZongertinibTier 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。

氟泽雷塞优化路线步数:9总收率:/
(aR)-6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-1,8-naphthyridin-2-one→6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-1,8-naphthyridin-2-one→(R)-Piperazine-1,3-dicarboxylic acid 1-tert-butyl 3-methyl diester→(aR)-6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-3-nitro-1,8-naphthyridin-2-one→(aR)-6,7-Dichloro-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-2-oxo-1,2-dihydro-1,8-naphthyridin-4-yl trifluoromethanesulfonate→(aR)-1-tert-Butyl 3-methyl (3R)-4-[6,7-dichloro-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-2-oxo-1,2-dihydro-1,8-naphthyridin-4-yl]piperazine-1,3-dicarboxylate→(aR)-tert-Butyl (4aR)-10,11-dichloro-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate→Dimethoxysulfone→(aR)-tert-Butyl (4aR)-10,11-dichloro-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate→(2-Fluoro-6-hydroxyphenyl)boronic acid→(aR)-tert-Butyl (4aR)-11-chloro-10-(2-fluoro-6-hydroxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate→(aR)-(4aR)-11-Chloro-10-(2-fluoro-6-hydroxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-2,3,4,4a,6,8-hexahydro-1H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-5,7-dione→2-Propenoyl chloride
宗艾替尼优化路线步数:5总收率:/
3-Methyl-4-((1-methyl-1H-benzimidazol-5-yl)oxy)benzenamine→1-Fluoro-2-methyl-4-nitrobenzene→4-Amino-3-nitrophenol→4-(2-Methyl-4-nitrophenoxy)-2-nitroaniline→Dimethoxysulfone→N-Methyl-4-(2-methyl-4-nitrophenoxy)-2-nitroaniline→4-(4-Amino-2-methylphenoxy)-N1-methylbenzene-1,2-diamine→Formic acid→N-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]formamide

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同 CAS 多家在售供应横向对比;价格区间为供应方挂牌口径,实价以询价确认为准。

供应商产品价格区间最小起订货期资质操作
Unibest Nantong cGMP Site4-Bromo-2-methoxybenzaldehyde
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Unibest Taizhou GMP-like Site4-formyl-3-methoxybenzonitrile
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Qualified Partner — East China API Works4-AMino-5-Methylpyridin-2-ol
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Unibest Nantong cGMP Site2-chloro-5-methylpyridin-4-amine
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Unibest Taizhou GMP-like Site2-Cyanoethyl 3-oxobutanoate
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Qualified Partner — East China API Works2-cyanoethyl 4-(4-cyano-2-methoxyphenyl)-2,8-dimethyl-5-oxo-1,4,5,6-tetrahydro-1,6-naphthyridine-3-carboxylate
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本页为中间体 CAS 注册档案:同 CAS 的多条路线登记已合并;后续供应商报价与买方需求以该 CAS 为主键撮合。