合成路线:By condensation of alpha-(4-ethyl-2,3-dioxo-1-piperazinocarbonylamino)-p-hydroxyphenylacetic acid (I) with 7-amino-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid (II) by means of ethyl chlorocarbonate and N,O-bis(trimethylsilyl)acetamide in acetonitrile.
合成路线:The condensation of N-(1-methoxycarbonyl-1-propen-2-yl)-alpha-amino-p-hydroxyphenylacetic sodium salt (III) with 7-amino-3-[(1-methyl-1H-tetrazol-5-yl) thiomethyl]-3-cephem-4-carboxylic acid (II) by means of ethyl chlorocarbonate and N,O-bis(trimethylsilyl)acetamide (A) in acetonitrile gives 7-(alpha-amino-p-hydroxy-phenylacetamido)-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid (IV),which is then condensed with 4-ethyl-2,3-dioxopiperazino-1-carbonyl chloride (V) by means of K2CO3 in ethyl acetate water.
合成路线:The condensation of alpha-(4-ethyl-2,3-dioxo-1-piperazinocarbonylamino)-p-hydroxyphenylacetic acid (I) with 7-amino-3-acetoxymethyl-3-cephem-4-carboxylic acid (VI) by means of ethyl chlorocarbonate and N,O-bis(trimethylsilyl)acetamide (A) gives the 3-acetoxymethyl derivate (VII),which is then condensed with 1-methyl-5-mercapto-1H-tetrazole (VIII) by means of NaHCO3 in a phosphate buffer.
合成路线:The condensation of acetoxymethyl derivative (VI) with N-(1-methoxycarbonyl-1-propen-2-yl)-alpha-amino-p-hydroxyphenylacetic sodium salt (III) by means of ethyl chlorocarbonate and N,O-bis(trimethylsilyl)acetamide (A) gives 7-(alpha-amino-p-hydroxyphenylacetamido)-3-acetoxymethyl-3-cephem-4-carboxylic acid (IX),which is then condensed with acyl chloride (V) by means of K2CO3 in ethyl acetate water to afford (VII),which is then condensed with 1-methyl-5-mercapto-1H-tetrazole (VIII) by means of NaHCO3 in a phosphate buffer.
合成路线:The condensation of (II) with the substituted phenylacetic acid (X) by means of ethyl chlorocarbonate gives the cephalosporin (XI),which is then cyclized by means of NaH in ethanol.
参考文献标题:T-1551
文献作者:Castar,J.; Serradell,M.N.; Blancafort,P.
参考来源:Drugs Fut 1979,4(9),675
合成路线:By condensation of alpha-(4-ethyl-2,3-dioxo-1-piperazinocarbonylamino)-p-hydroxyphenylacetic acid (I) with 7-amino-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid (II) by means of ethyl chlorocarbonate and N,O-bis(trimethylsilyl)acetamide in acetonitrile.
合成路线:The condensation of N-(1-methoxycarbonyl-1-propen-2-yl)-alpha-amino-p-hydroxyphenylacetic sodium salt (III) with 7-amino-3-[(1-methyl-1H-tetrazol-5-yl) thiomethyl]-3-cephem-4-carboxylic acid (II) by means of ethyl chlorocarbonate and N,O-bis(trimethylsilyl)acetamide (A) in acetonitrile gives 7-(alpha-amino-p-hydroxy-phenylacetamido)-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid (IV),which is then condensed with 4-ethyl-2,3-dioxopiperazino-1-carbonyl chloride (V) by means of K2CO3 in ethyl acetate water.
合成路线:The condensation of alpha-(4-ethyl-2,3-dioxo-1-piperazinocarbonylamino)-p-hydroxyphenylacetic acid (I) with 7-amino-3-acetoxymethyl-3-cephem-4-carboxylic acid (VI) by means of ethyl chlorocarbonate and N,O-bis(trimethylsilyl)acetamide (A) gives the 3-acetoxymethyl derivate (VII),which is then condensed with 1-methyl-5-mercapto-1H-tetrazole (VIII) by means of NaHCO3 in a phosphate buffer.
合成路线:The condensation of acetoxymethyl derivative (VI) with N-(1-methoxycarbonyl-1-propen-2-yl)-alpha-amino-p-hydroxyphenylacetic sodium salt (III) by means of ethyl chlorocarbonate and N,O-bis(trimethylsilyl)acetamide (A) gives 7-(alpha-amino-p-hydroxyphenylacetamido)-3-acetoxymethyl-3-cephem-4-carboxylic acid (IX),which is then condensed with acyl chloride (V) by means of K2CO3 in ethyl acetate water to afford (VII),which is then condensed with 1-methyl-5-mercapto-1H-tetrazole (VIII) by means of NaHCO3 in a phosphate buffer.
参考文献标题:Nouvelles c閜haslosporines,leur proc閐?de pr閜aration et leur application en th閞apeutique
文献作者:Saikawa,I.; et al.
参考来源:BE 0837682
产品链接: CAS No. 62893-20-3›› 产品链接: CAS No.62893-19-0››