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CAS 438631-77-7
(R)-Piperazine-1,3-dicarboxylic acid 1-tert-butyl 3-methyl diester
登记编号：(VII)1225102-1-a、(XIX)1225102-2-b
应用背景（按来源药适应症）
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
来源药（使用该中间体的合成路线）
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 氟泽雷塞Fulzerasib | Tier 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。
6,7-Dichloro-1,2-dihydro-4-hydroxy-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-2-oxo-1,8-naphthyridine-3-carbonitrile→6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-1,8-naphthyridin-2-one→6,7-Dichloro-4-hydroxy-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-1,8-naphthyridin-2(1H)-one→(2-Fluoro-6-methoxyphenyl)boronic acid→6-Chloro-7-(2-fluoro-6-methoxyphenyl)-4-hydroxy-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-1,8-naphthyridin-2(1H)-one→4,6-Dichloro-7-(2-fluoro-6-methoxyphenyl)-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-1,8-naphthyridin-2(1H)-one→(R)-Piperazine-1,3-dicarboxylic acid 1-tert-butyl 3-methyl diester→1-tert-Butyl 3-methyl (3R)-4-[6-chloro-7-(2-fluoro-6-methoxyphenyl)-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→tert-Butyl (4aR)-11-chloro-10-(2-fluoro-6-methoxyphenyl)-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→Iodomethane→tert-Butyl (4aR)-11-chloro-10-(2-fluoro-6-methoxyphenyl)-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)-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
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