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Preparation of beta-lactam derivatives used as antibacterial agents by reacting cephalosporanic acid derivative with imine compound, then thiourea compound
Preparation of beta-lactam derivatives used as antibacterial agents by reacting cephalosporanic acid derivative with imine compound, then thiourea compound
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机译:通过使头孢烷酸衍生物与亚胺化合物然后与硫脲化合物反应来制备用作抗菌剂的β-内酰胺衍生物
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摘要
Preparation of beta -lactam derivatives (I) comprises: (1) reacting a cephalosporanic acid derivative (IV) with an imine derivative (III) and (2) reacting the obtained compound (II) with a thioether compound (V) to give a compound (VI) which is then desilylated to give (I) or (3) desilylating (II) and reacting with thiourea in a solvent system containing organic solvent and water to give (I). Preparation of beta -lactam derivatives of formula (I) comprises: (1) reacting a cephalosporanic acid derivative of formula (IV) with an imine derivative of formula (III) and (2) reacting the obtained compound of formula (II) with a thioether compound of formula (V) to give a compound (VI) which is then desilylated to give (I) or (3) desilylating (II) and reacting with thiourea in a solvent system containing organic solvent and water to give (I). [Image] [Image] X, R1substituents useful in cephalosporin chemistry; REa negative charge or COOREan ester; R : H or silyl; RE'silyl or COORE'an ester; Y : halo; Y' : a group forming a reactive compound (III); R' : H or silyl and R'' : silyl. An independent claim is included for new compounds of formula (VIa). [Image] R'a, RE'a, R'''atri-1-4C alkylsilyl. ACTIVITY : Antibacterial. No biological data is given. MECHANISM OF ACTION : None given.
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