摘要:
A 2-substituted cephem derivative represented by the formula ##STR1## wherein R.sup.1 represents a substituted or unsubstituted phenyl group, substituted or unsubstituted phenylmethyl group or substituted or unsubstituted phenoxymethyl group, R.sup.2 represents hydrogen atom or protective group for carboxylic acid and Y represents allyloxy group, benzyloxy group, alkylthio group, carboxyalkylthio group or group of the formula ##STR2## wherein R.sup.4 represents hydrogen atom or lower alkyl group, X represents --O--, --S-- or ##STR3## R.sup.5 represents hydrogen atom, a lower alkyl group or phenyl group and R.sup.6 represents hydrogen atom or lower alkyl group, and a process for preparing the derivatives.
摘要:
An object of the invention is to provide a process for preparing a 3-substituted cephem compound from an allenyl-.beta.-lactam compound which can be easily produced from an inexpensive penicillin compound by a simple reaction procedure.The process of the invention comprises reacting an allenyl-.beta.-lactam compound with an organohalogen compound in the presence of a metal having a standard oxidation-reduction potential of -0.3 (V/SCE) or less in an amount at least equimolar with the allenyl-.beta.-lactam compound and 0.0001 to 0.5 mole, per mole of the allenyl-.beta.-lactam compound, of a metal compound having a higher standard oxidation-reduction potential than said metal.
摘要:
The present invention provides a process for preparing a cephem derivative characterized in that an allenyl .beta.-lactam compound represented by the formula (1) ##STR1## wherein R.sup.1 is amino or protected amino, R.sup.2 is a hydrogen atom or lower alkoxyl, R.sup.3 is a hydrogen atom or carboxylic acid protecting group and X is the group --SO.sub.2 R.sup.4 or --SR.sup.4, R.sup.4 being substituted or unsubstituted aryl or substituted or unsubstituted nitrogen-containing aromatic heterocyclic group is reacted with a nucleophilic agent to obtain the derivative, the cephem derivative being represented by the formula (2) ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, and Y is the residue of the nucleophilic agent.
摘要:
The present invention provides a process for preparing a 2-exo-methylenepenam derivative represented by the formula (2), the process being characterized by reacting an allenyl .beta.-lactum compound represented by the formula (1) with a metallic reducing agent, in which R.sup.1, R.sup.2, R.sup.3 and X are defined in the specification. ##STR1##
摘要:
A process for preparing an azetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is hydrogen, halogen or lower alkoxy, R.sup.2 is hydrogen, halogen, lower alkoxy, amino or a group ##STR2## (in which R.sup.5 is substituted or unsubstituted phenyl, substituted or unsubstituted phenylmethyl, substituted or unsubstituted phenoxymethyl, or substituted or unsubstituted benzoyl), or R.sup.1 and R.sup.2, when taken together, are carbonyl, R.sup.3 is substituted or unsubstituted phenyl, and R.sup.4 is hydrogen, optionally substituted hydrocarbon residue or acyl, silyl, sulfonyl or phosphonyl derived from inorganic acid or organic acid, the process comprising reacting a dithioazetidinone derivative represented by the formula ##STR3## wherein R.sup.1, R.sup.2 and R.sup.4 are as defined above and R.sup.9 is substituted or unsubstituted, nitrogen-containing aromatic heterocyclic residue with a compound represented by the formulaR.sup.3 SO.sub.2 H (VII)wherein R.sup.3 is defined above.
摘要:
This invention provides thiazolinoazetidinone derivatives represented by the formula ##STR1## and processes for preparing the same. The thiazolinoazetidinone derivatives are used as the intermediates for producing cephalosporin compounds useful as antibiotic agents.
摘要:
This invention provides a process for preparing a 2,2-bishalomethylpenam derivative represented by the formula ##STR1## wherein R.sup.1 represents a lower alkyl group, aryl group, arylmethyl group, arylcarbonyl group or aryloxymethyl group, R.sup.2 represents a carboxyl-protecting group, X.sup.1 and X.sup.2 are the same or different and represent a halogen atom, the process being characterized in that a disulfide represented by the formula ##STR2## wherein R.sup.1, R.sup.2 and X.sup.1 are as defined above and R.sup.3 represents an aryl group or heterocyclic group is subjected to an electrolytic reaction in a solvent in the presence of a halogen acid and/or halogen salt.
摘要:
This invention provides a process for preparing a .beta.-lactam derivative represented by the formula ##STR1## wherein R.sup.1 represents aralkyl group or aryloxy methyl group, Y represents the group ##STR2## (wherein R.sup.2 represents aryl-substituted lower alkyl group, aryloxy-substituted lower alkyl group or lower alkyl group optionally substituted with halogen atom and X represents halogen atom) or the group ##STR3## (wherein R.sup.2 and X are as defined above), the process comprising electrolyzing an azetidinone derivative of the formula ##STR4## wherein R.sup.1 and R.sup.2 are as defined above in the presence of hydrohalogenic acid and/or halide.
摘要:
This invention provides a process for preparing an oxazolineazetidinone derivative represented by the formula ##STR1## (wherein R.sup.1 represents hydrogen atom, alkyl group, alkenyl group, substituted or unsubstituted aralkyl group, substituted or unsubstituted aryl group, or substituted or unsubstituted aryloxymethyl group, R.sup.2 represents free or protected carboxyl group and R.sup.3 represents hydrogen atom or methoxy group) from a penicillin derivative represented by the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sub.3 are as defined above.
摘要:
The present invention provides a thiazolinoazetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is phenyl having or not having substituent(s), methyl having or not having substituent(s) or ##STR2## group, R.sup.3 being phenyl having or not having substituent(s), and R.sup.2 is a hydrogen atom or carboxylic acid protective group, and a process for preparing the same.The present invention further provides a process for preparing a 2-exo-methylenepenam derivative characterized by hydrolyzing the thiazoline ring of a thiazolinoazetidinone derivative of the above formula (1) to effect recyclization and obtain a 2-exo-methylenepenam derivative represented by the formula ##STR3## wherein R.sup.1 and R.sup.2 are as defined above.