Blau Lorena, Menegon Renato Farina, Ferreira Elizabeth Igne, Ferreira Antonio Gilberto, Boffo Elisangela Fabiana, Tavares Leila Aley, Heleno Vladimir Constantino Gomes, Chung Man-Chin
Departamento de Fármacos e Medicamentos, Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, CP 502 - 14801-902, Araraquara, SP, Brazil.
Molecules. 2008 Apr 10;13(4):841-54. doi: 10.3390/molecules13040841.
We report the synthesis and total NMR characterization of 5-thia-1-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid-3-[[[(4''-nitrophenoxy)carbonyl]oxy]-methyl]-8-oxo-7-[(2-thienyloxoacetyl)amino]-diphenylmethyl ester-5-dioxide (5), a new cephalosporin derivative. This compound can be used as the carrier of a wide range of drugs containing an amino group. The preparation of the intermediate product, 5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid-3-[methyl 4-(6-methoxyquinolin-8-ylamino)pentylcarbamate]-8-oxo-7-[(2-thienyloxoacetyl)amino]-diphenylmethyl ester-5-dioxide (6), as well as the synthesis of the antimalarial primaquine prodrug 5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid-3-[methyl 4-(6-methoxyquinolin-8-ylamino)pentylcarbamate]-8-oxo-7-[(2-thienyloxoacetyl)amino]- 5-dioxide (7) are also described, together with their total (1)H- and (13)C-NMR assignments.
我们报道了一种新型头孢菌素衍生物5-硫杂-1-氮杂双环-[4.2.0]辛-2-烯-2-羧酸-3-[[[(4''-硝基苯氧基)羰基]氧基]-甲基]-8-氧代-7-[(2-噻吩基氧乙酰基)氨基]-二苯甲酯-5-二氧化物（5）的合成及全核磁共振表征。该化合物可用作多种含氨基药物的载体。还描述了中间体产物5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸-3-[甲基4-(6-甲氧基喹啉-8-基氨基)戊基氨基甲酸酯]-8-氧代-7-[(2-噻吩基氧乙酰基)氨基]-二苯甲酯-5-二氧化物（6）的制备，以及抗疟原药伯氨喹前药5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸-3-[甲基4-(6-甲氧基喹啉-8-基氨基)戊基氨基甲酸酯]-8-氧代-7-[(2-噻吩基氧乙酰基)氨基]-5-二氧化物（7）的合成，以及它们的全氢谱和碳谱核磁共振归属。
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