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CAS 5469-69-2
6-chloropyridazin-3-amine
登记编号:RELU-010、ENSAR-002、RISD-031、GAND-001
应用背景(按来源药适应症)
前列腺癌瑞卢戈利平滑肌瘤瑞卢戈利非小细胞肺癌盐酸恩沙替尼肺癌盐酸恩沙替尼脑转移盐酸恩沙替尼非霍奇金淋巴瘤盐酸恩沙替尼肝胚细胞瘤盐酸恩沙替尼骨肉瘤盐酸恩沙替尼脊髓性肌萎缩利司扑兰血液肿瘤Gandotinib骨髓纤维化Gandotinib骨髓增生性疾病Gandotinib原发性血小板增多症Gandotinib真性红细胞增多症Gandotinib
来源药(使用该中间体的合成路线)
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 瑞卢戈利Relugolix | Tier C · 观察 / 贸易 | 2031 |
| 盐酸恩沙替尼Ensartinib Hydrochloride | Tier C · 观察 / 贸易 | - |
| 利司扑兰Risdiplam | Tier B · 提前布局 | - |
| Gandotinib | 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。
ethyl 2-amino-4-methyl-5-(4-nitrophenyl)thiophene-3-carboxylate→ethyl 2-((ethoxycarbonyl)amino)-4-methyl-5-(4-nitrophenyl)thiophene-3-carboxylate→2-(chloromethyl)-1,3-difluorobenzene→ethyl 2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-4-methyl-5-(4-nitrophenyl)thiophene-3-carboxylate→ethyl 4-(bromomethyl)-2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-5-(4-nitrophenyl)thiophene-3-carboxylate→ethyl 2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-4-(((2-methoxyethyl)(methyl)amino)methyl)-5-(4-nitrophenyl)thiophene-3-carboxylate→ethyl 5-(4-aminophenyl)-2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-4-(((2-methoxyethyl)(methyl)amino)methyl)thiophene-3-carboxylate→ethyl 2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-4-(((2-methoxyethyl)(methyl)amino)methyl)-5-(4-(3-methoxyureido)phenyl)thiophene-3-carboxylate→2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-4-(((2-methoxyethyl)(methyl)amino)methyl)-5-(4-(3-methoxyureido)phenyl)thiophene-3-carboxylic acid→6-chloropyridazin-3-amine→1-(4-(1-(2,6-difluorobenzyl)-5-(((2-methoxyethyl)(methyl)amino)methyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea→1-chloroethyl carbonochloridate
3,6-dichloropyridazine→6-chloropyridazin-3-amine→4-bromo-6-chloropyridazin-3-amine→1-(2,6-dichloro-3-fluorophenyl)ethan-1-ol→(R)-6-chloro-4-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridazin-3-amine→ENSAR-006→ENSAR-007→ENSAR-008→methyl 4-aminobenzoate→ENSAR-010→ENSAR-011→(2R,6S)-2,6-dimethylpiperazine→ENSAR-013→1-(2,6-dichloro-3-fluorophenyl)ethan-1-ol
1-aminocyclopropanecarboxylic acid→ethyl 1-aminocyclopropanecarboxylate hydrochloride→2-chloroacetyl chloride→ethyl 1-(2-chloroacetamido)cyclopropanecarboxylate→7-benzyl-4,7-diazaspiro[2.5]octane-5,8-dione→7-benzyl-4,7-diazaspiro[2.5]octane→tert-butyl 7-benzyl-4,7-diazaspiro[2.5]octane-4-carboxylate→oxalic acid→tert-butyl 4,7-diazaspiro[2.5]octane-4-carboxylate hemioxalate→tert-butyl 4,7-diazaspiro[2.5]octane-4-carboxylate→5-bromo-2-chloropyridine→tert-butyl 7-(6-chloropyridin-3-yl)-4,7-diazaspiro[2.5]octane-4-carboxylate→tert-butyl 7-(6-aminopyridin-3-yl)-4,7-diazaspiro[2.5]octane-4-carboxylate→di-tert-butyl malonate→tert-butyl 7-(2-hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidin-7-yl)-4,7-diazaspiro[2.5]octane-4-carboxylate→tert-butyl 7-(4-oxo-2-(tosyloxy)-4H-pyrido[1,2-a]pyrimidin-7-yl)-4,7-diazaspiro[2.5]octane-4-carboxylate→2,8-dimethyl-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)imidazo[1,2-b]pyridazine→tert-butyl 7-(2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-7-yl)-4,7-diazaspiro[2.5]octane-4-carboxylate→6-chloropyridazin-3-amine→4-bromo-6-chloropyridazin-3-amine→6-chloro-4-methylpyridazin-3-amine→isopropyl acetate→6-chloro-2,8-dimethylimidazo[1,2-b]pyridazine
6-chloropyridazin-3-amine→1,1-dimethoxy-N,N-dimethylethanamine→(E)-N'-(6-chloropyridazin-3-yl)-N,N-dimethylacetimidamide→2-chloro-1-(4-chloro-2-fluorophenyl)ethanone→(4-chloro-2-fluorophenyl)(6-chloro-2-methylimidazo[1,2-b]pyridazin-3-yl)methanone→(4-chloro-2-fluorophenyl)(6-chloro-2-methyl-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-3-yl)methanone→4-((6-chloro-3-(4-chloro-2-fluorobenzyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)methyl)morpholine→1-(tert-butyl)-3-methyl-1H-pyrazol-5-amine→3-(4-chloro-2-fluorobenzyl)-N-(1-(4-methoxybenzyl)-3-methyl-1H-pyrazol-5-yl)-2-methyl-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine→1-(4-chloro-2-fluorophenyl)ethanone→tert-butylhydrazine hydrochloride→(E)-3-aminobut-2-enenitrile→3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine
6-chloropyridazin-3-amine→4-((6-chloro-3-(4-chloro-2-fluorobenzyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)methyl)morpholine→ethyl 2-chloro-3-oxobutanoate→ethyl 6-chloro-2-methylimidazo[1,2-b]pyridazine-3-carboxylate→ethyl 6-chloro-2-methyl-8-(morpholinomethyl)imidazo[1,2-b]pyridazine-3-carboxylate→4-((6-chloro-2-methylimidazo[1,2-b]pyridazin-8-yl)methyl)morpholine→4-((6-chloro-2-methylimidazo[1,2-b]pyridazin-8-yl)methyl)morpholine
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