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CAS 73616-27-0

2-(5-Amino-1H-pyrazol-1-yl)ethan-1-ol

登记编号:Cefoselis Sulfate-001

应用背景(按来源药适应症)

细菌感染硫酸头孢噻利

来源药(使用该中间体的合成路线)

品种梯队到期年
硫酸头孢噻利Cefoselis SulfateTier C · 观察 / 贸易-

合成路线中的位置(上下游链)

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硫酸头孢噻利优化路线步数:7总收率:6.53g(Cefoselis Sulfate (API))
2-(5-Amino-1H-pyrazol-1-yl)ethan-1-ol→2-[5-(Formylamino)-1H-pyrazol-1-yl]ethyl formate→Diphenylmethyl (6R,7R)-7-[(tert-butoxycarbonyl)amino]-3-(chloromethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate→2-([(6R,7R)-7-[(tert-Butoxycarbonyl)amino]-2-[(diphenylmethoxy)carbonyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl)-5-(formylamino)-1-[2-(formyloxy)ethyl]-1H-pyrazol-2-ium iodide→(6R,7R)-7-Amino-3-[[5-amino-1-(2-hydroxyethyl)-1H-pyrazol-2-ium-2-yl]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate hydrochloride→(2Z)-[2-(Formylamino)-1,3-thiazol-4-yl](methoxyimino)ethanoic acid→(6R,7R)-3-[[5-Amino-1-(2-hydroxyethyl)-1H-pyrazol-2-ium-2-yl]methyl]-7-[[(2Z)-2-[2-(formylamino)-1,3-thiazol-4-yl]-2-(methoxyimino)acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate→(6R,7R)-3-[[5-Amino-1-(2-hydroxyethyl)-1H-pyrazol-2-ium-2-yl]methyl]-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate→1-[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]-3-oxido-1H-1,2,3-benzotriazol-3-ium
硫酸头孢噻利优化路线步数:10总收率:231. 2g(Cefoselis Sulfate-001)
2-(5-Amino-1H-pyrazol-1-yl)ethan-1-ol→N,N-Dimethylformamide→2-Cyanoacetic acid methyl ester→2-Cyanoacetic acid ethyl ester→Propyl cyanoacetate→Butyl cyanoacetate→Methyl 2-cyano-3-(dimethylamino)prop-2-enoate→Ethyl 2-cyano-3-(dimethylamino)prop-2-enoate→Propyl 2-cyano-3-(dimethylamino)prop-2-enoate→Butyl 2-cyano-3-(dimethylamino)prop-2-enoate→2-Hydrazinoethanol→Methyl 5-amino-1-(2-hydroxyethyl)-1H-pyrazole-4-carboxylate→Ethyl 5-amino-1-(2-hydroxyethyl)-1H-pyrazole-4-carboxylate→Propyl 5-amino-1-(2-hydroxyethyl)-1H-pyrazole-4-carboxylate→Butyl 5-amino-1-(2-hydroxyethyl)-1H-pyrazole-4-carboxylate→5-Amino-1-(2-hydroxyethyl)-1H-pyrazole-4-carboxylic acid→Hex-3-enedinitrile→But-3-enenitrile→3-Oxopropanenitrile→3,3-Dimethoxypropanenitrile→3-[2-(2-Hydroxyethyl)hydrazinylidene]propanenitrile

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