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CAS 38496-18-3
2,6-Dichloronicotinic acid2,6-Dichloropyridine-3-carboxylic acid2,6-dichloronicotinic acid
登记编号:(I)1225102-2-a、(III)965082-1-a、CX-5461-001、(I)1114845-3-a
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边缘带B细胞淋巴瘤奥布替尼套细胞淋巴瘤奥布替尼慢性淋巴细胞白血病奥布替尼特发性血小板减少性紫癜奥布替尼系统性红斑狼疮奥布替尼多发性硬化奥布替尼结直肠癌Pidnarulex实体瘤PidnarulexBurkitt淋巴瘤PidnarulexB-细胞淋巴瘤Pidnarulex淋巴瘤PidnarulexHR阳性乳腺癌Pidnarulex非小细胞肺癌格索雷塞结直肠癌格索雷塞实体瘤格索雷塞肾细胞癌格索雷塞胰腺癌格索雷塞
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 | - |
| 奥布替尼Orelabrutinib | Tier C · 观察 / 贸易 | - |
| Pidnarulex | Tier C · 观察 / 贸易 | - |
| 格索雷塞Garsorasib | 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。
2,6-Dichloronicotinic acid→2-Isopropyl-4-methylpyridin-3-amine→6-Chloro-2-[(2-isopropyl-4-methyl-3-pyridyl)amino]pyridine-3-carboxylic acid→5,6-Dichloro-2-[(2-isopropyl-4-methyl-3-pyridyl)amino]pyridine-3-carboxylic acid→5,6-Dichloro-2-[[4-methyl-2-(propan-2-yl)pyridin-3-yl]amino]pyridine-3-carbonyl chloride→3-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-oxopropanoic acid→(alphaR)-alpha-Methyl-3,5-bis(trifluoromethyl)benzenemethanol→2,2-Dimethyl-1,3-dioxane-4,6-dione→3-Oxo-3-[(1S)-1-phenylethoxy]propanoic acid→(1S)-Methyl phenyl carbinol→(1S)-1-[3,5-Bis(trifluoromethyl)phenyl]ethyl 3-(5,6-dichloro-2-[[4-methyl-2-(propan-2-yl)pyridin-3-yl]amino]pyridin-3-yl)-3-oxopropanoate→(1S)-1-Phenylethyl 3-(5,6-dichloro-2-[[4-methyl-2-(propan-2-yl)pyridin-3-yl]amino]pyridin-3-yl)-3-oxopropanoate→6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-1,8-naphthyridin-2-one→3-[(1R,2S,5R)-2-Isopropyl-5-methylcyclohexoxy]-3-oxo-propanoic acid→(-)-(1R-(1-alpha,2-beta,5-alpha))-5-Methyl-2-(1-methylethyl)cyclohexanol→(1R,2S,5R)-5-Methyl-2-(propan-2-yl)cyclohexyl 3-(5,6-dichloro-2-[[4-methyl-2-(propan-2-yl)pyridin-3-yl]amino]pyridin-3-yl)-3-oxopropanoate
2,6-Dichloronicotinonitrile→2,6-Dichloronicotinamide→2,6-Dichloropyridine-3-carboxylic acid→(3-Phenoxyphenyl)boronic acid→4,4,5,5-Tetramethyl-2-(3-phenoxyphenyl)-1,3,2-dioxaborolane→6-Chloro-2-(4-phenoxyphenyl)pyridine-3-carboxamide→N-Boc-1,2,5,6-tetrahydropyridine-4-boronic acid pinacol ester→tert-Butyl 5-carbamoyl-6-(4-phenoxyphenyl)-3',6'-dihydro[2,4'-bipyridine]-1'(2'H)-carboxylate→tert-Butyl 4-[5-carbamoyl-6-(4-phenoxyphenyl)pyridin-2-yl]piperidine-1-carboxylate→2-(4-Phenoxyphenyl)-6-(piperidin-4-yl)pyridine-3-carboxamide→2-(4-Phenoxyphenyl)-6-(piperidin-4-yl)pyridine-3-carboxamide hydrogen chloride→Acryloyl chloride
2-(4-methyl-1,4-diazepan-1-yl)-N-((5-methylpyrazin-2-yl)methyl)-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxamide→2,6-dichloronicotinic acid→2,6-dichloronicotinoyl chloride→ethyl 2-(benzo[d]thiazol-2-yl)acetate→ethyl 2-chloro-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxylate→1-methyl-1,4-diazepane→ethyl 2-(4-methyl-1,4-diazepan-1-yl)-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxylate→(5-methylpyrazin-2-yl)methanamine
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