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CAS 110-86-1
AzabenzenepyridinePyridine
登记编号:(I)461018-26-a、Ceftazidime-014、DALF-001、Folic Acid-012、Dalpiciclib Isethionate-025、MONT-013
应用背景(按来源药适应症)
华氏巨球蛋白血症伊布替尼慢性淋巴细胞白血病伊布替尼套细胞淋巴瘤伊布替尼移植物抗宿主病伊布替尼膀胱炎阿维巴坦钠/头孢他啶胆囊炎阿维巴坦钠/头孢他啶腹膜炎阿维巴坦钠/头孢他啶腹腔感染阿维巴坦钠/头孢他啶肝脓肿阿维巴坦钠/头孢他啶脓毒病阿维巴坦钠/头孢他啶细菌感染头孢他啶/他唑巴坦钠呼吸道感染头孢他啶/他唑巴坦钠泌尿系统感染头孢他啶/他唑巴坦钠多发性硬化达伐吡啶脊髓小脑共济失调达伐吡啶短时记忆达伐吡啶挤压伤达伐吡啶周围神经损伤达伐吡啶脊髓损伤达伐吡啶原发性高血压马来酸依那普利/叶酸细菌感染头孢他啶革兰氏阳性细菌感染头孢他啶革兰氏阴性细菌感染头孢他啶妇科疾病头孢他啶腹腔感染头孢他啶骨关节炎头孢他啶巨幼红细胞性贫血叶酸叶酸缺乏叶酸神经管缺损叶酸贫血叶酸热潮红叶酸高同型半胱氨酸血症叶酸乳腺癌羟乙磺酸达尔西利转移性乳腺癌羟乙磺酸达尔西利前列腺癌羟乙磺酸达尔西利三阴性乳腺癌羟乙磺酸达尔西利脑膜瘤羟乙磺酸达尔西利肝功能衰退羟乙磺酸达尔西利过敏性鼻炎孟鲁司特钠哮喘孟鲁司特钠超敏反应孟鲁司特钠季节性过敏性鼻炎孟鲁司特钠常年性变应性鼻炎孟鲁司特钠运动诱发哮喘孟鲁司特钠
来源药(使用该中间体的合成路线)
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 伊布替尼Ibrutinib | Tier A · 立即攻坚 | 2027 |
| 阿维巴坦钠/头孢他啶Avibactam Sodium/Ceftazidime | Tier C · 观察 / 贸易 | - |
| 头孢他啶/他唑巴坦钠Ceftazidime/Tazobactam Sodium | Tier C · 观察 / 贸易 | - |
| 达伐吡啶Dalfampridine | Tier C · 观察 / 贸易 | - |
| 马来酸依那普利/叶酸Enalapril Maleate/Folic Acid | Tier C · 观察 / 贸易 | - |
| 头孢他啶Ceftazidime | Tier C · 观察 / 贸易 | - |
| 叶酸Folic Acid | Tier C · 观察 / 贸易 | - |
| 羟乙磺酸达尔西利Dalpiciclib Isethionate | Tier C · 观察 / 贸易 | - |
| 孟鲁司特钠Montelukast | Tier B · 提前布局 | - |
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。
Azabenzene→3-Pyridylsulfonic acid→3-Hydroxypyridine→3-Hydroxypiperidine→(2S,3S)-4-[(4-Chlorophenyl)amino]-2,3-dihydroxy-4-oxobutanoic acid (3S)-piperidin-3-ol→1-(Phenylmethyl)-3-piperidinol→(2S,3S)-4-((4-Chlorophenyl)amino)-2,3-dihydroxy-4-oxobutanoic acid→(2S,3S)-(-)-Tartaric acid→1-Amino-4-chlorobenzene→(3S)-1-(tert-Butoxycarbonyl)-3-hydroxypiperidine
ethyl 3-oxobutanoate→Ethyl nitrite→Non-denatured ethanol→ethyl (E)-2-(hydroxyimino)-3-oxobutanoate→thiourea→ethyl (Z)-2-(2-aminothiazol-4-yl)-2-(hydroxyimino)acetate→Ethyl (2Z)-(hydroxyimino)[2-[(triphenylmethyl)amino]-1,3-thiazol-4-yl]acetate→tert-Butyl 2-bromo-2-methylpropionate→tert-Butyl 2-[[(Z)-(2-ethoxy-2-oxo-1-[2-[(triphenylmethyl)amino]-1,3-thiazol-4-yl]ethylidene)amino]oxy]-2-methylpropanoate→(2Z)-[[(1-tert-Butoxy-2-methyl-1-oxopropan-2-yl)oxy]imino][2-[(triphenylmethyl)amino]-1,3-thiazol-4-yl]acetic acid→(6R,7R)-3-(Acetoxymethyl)-7-amino-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid→(6R,7R)-3-[(Acetyloxy)methyl]-7-[[(2Z)-2-[[(1-tert-butoxy-2-methyl-1-oxopropan-2-yl)oxy]imino]-2-[2-[(triphenylmethyl)amino]-1,3-thiazol-4-yl]acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid→(6R,7R)-3-[(Acetyloxy)methyl]-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-[[(2-carboxypropan-2-yl)oxy]imino]acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid→pyridine
(6R,7R)-3-(Acetoxymethyl)-7-amino-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid→Trimethylsilyl 7-(trimethylsilylamino)cephalosporanate→Trimethylsilyl (6R,7R)-3-(iodomethyl)-8-oxo-7-[(trimethylsilyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate→Pyridine→1-[[(6R,7R)-8-Oxo-7-[(trimethylsilyl)amino]-2-[[(trimethylsilyl)oxy]carbonyl]-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]pyridin-1-ium iodide→(6R,7R)-7-Amino-8-oxo-3-(pyridinium-1-ylmethyl)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate dihydrochloride→2-[[(Z)-[1-(2-Amino-1,3-thiazol-4-yl)-2-[(1,3-benzothiazol-2-yl)sulfanyl]-2-oxoethylidene]amino]oxy]-2-methylpropanoic acid→tert-Butyl 2-[[(Z)-[1-(2-amino-1,3-thiazol-4-yl)-2-[(1,3-benzothiazol-2-yl)sulfanyl]-2-oxoethylidene]amino]oxy]-2-methylpropanoate→(6R,7R)-7-[[(2Z)-2-(2-Amino-1,3-thiazol-4-yl)-2-[[(1-tert-butoxy-2-methyl-1-oxopropan-2-yl)oxy]imino]acetyl]amino]-8-oxo-3-[(pyridin-1-ium-1-yl)methyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylat e
4-(Dimethylamino)phenol→tert-Butyl (5Z)-5-(2-amino-1,3-thiazol-4-yl)-8,8-dimethyl-4-oxo-3,7-dioxa-2-thia-6-azanon-5-en-9-oate 2,2-dioxide→4-Methoxybenzyl (6R,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-[[(1-tert-butoxy-2-methyl-1-oxopropan-2-yl)oxy]imino]acetyl]amino]-3-(chloromethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate→1-[[(6R,7R)-7-[[(2Z)-2-(2-Amino-1,3-thiazol-4-yl)-2-[[(1-tert-butoxy-2-methyl-1-oxopropan-2-yl)oxy]imino]acetyl]amino]-2-[[(4-methoxybenzyl)oxy]carbonyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]pyridinium chloride→4-Hydroxyaniline→(2Z)-(2-Amino-1,3-thiazol-4-yl)[[(1-tert-butoxy-2-methyl-1-oxopropan-2-yl)oxy]imino]acetic acid→Pyridine→4-Methoxybenzyl (6R,7R)-7-amino-3-(chloromethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate hydrochloride
Pyridine hydrobromide→Pyridine
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