摘要:
2α-Methyl-2β-(1,2,3-triazol-1-yl)methylpenam-3α-carboxylic acid derivatives are prepared by reacting a penicillanic acid sulfoxide derivative of the formula wherein R is a penicillin carboxyl protecting group, and R₁ is hydrogen or halogen, R₂ is hydrogen, lower alkyl or the like with a triazole derivative of the formula wherein R₃ and R₄ are hydrogen, trialkylsilyl, lower alkyl, lower alkoxy or the like and R₅ is hydrogen or silyl substituted with 3 groups selected from the class consisting of lower alkyl, benzyl and phenyl in a solvent.
摘要翻译:2α-甲基-2β-(1,2,3-三唑-1-基)甲基亚磺酸-3α-羧酸衍生物通过使式的青霉烷酸亚砜衍生物,其中R是青霉素羧基 R 1为氢或卤素,R 2为氢,低级烷基等与式CHEM的三唑衍生物反应,其中R 3和R 4为氢,三烷基甲硅烷基,低级烷基,低级烷氧基等,R 5为氢 或在溶剂中由选自低级烷基,苄基和苯基的3种基团取代的甲硅烷基。
摘要:
A process for preparing a 2β-substituted-methylpenicillin compound of the formula wherein -N Y is an optionally substituted heterocyclic group containing 2 to 4 nitrogen atoms as the hetero atom in the ring structure, and R₁ is a penicillin carboxyl protecting group, the process comprising reacting an azetidinonedisulfide compound of the formula wherein R₁ is as defined above and R is a substituted or unsubstituted heterocyclic group with a nitrogen-containing heterocyclic compound of the formula wherein is as defined above in the presence of a metal compound.
摘要:
The present invention provides a process for preparing a penicillanic acid derivative of the formula which comprises reacting lead with a halogenated penicillanic acid derivative of the formula wherein X, Y, Z and R¹ are defined in the specification. The reaction is conducted more advantageously in the presence of a metal having higher ionization tendency than lead.
摘要:
Disclosed is a process for preparing 2β-substituted-methylpenicillin derivative of the formula wherein R is H or carboxyl protecting group, R 1 is H or halo, R 2 is H, lower alkyl. lower alkoxy, halogen. azido, lower alkylthio, phthalimide or a group -NHR 3 (wherein R 3 is H or acyl), and - is an optionally substituted monocyclic or bicyclic heterocyclic group having 1 to 4 nitrogen atoms in the ring structure, the process comprising reacting a compound of the formula wherein X is Cl or Br, and R, R 1 and R 2 are as defined above with a heterocyclic compound of the formula
摘要:
The present invention provides a process for for preparing an exo-methylenepenam compound represented by the general formula (5) characterized in that a β -lactam halide compound represented by the general formula (2) is reduced with a metal having a standard oxidation-reduction potential of up to -0.3 (V/SCE) in an amount of at least one mole per mole of the halide compound and with a metal compound having a higher standard oxidation-reduction potential than the metal in an amount of 0.0001 to 10 moles per mole of the halide compound, or is subjected to an electroreduction process to obtain the exo-methylenepenam compound.