摘要:
This invention provides a process for preparing a thiosulfonate derivative represented by the formulaR.sup.2 SO.sub.2 SR.sup.1 (III)wherein R.sup.1 is substituted or unsubstituted 2-benzothiazolyl, and R.sup.2 is substituted or unsubstituted phenyl, the process being characterized in that a compound represented by the formulaR.sup.1 SX (I)wherein R.sup.1 is as defined above, and X is hydrogen, alkali metal or SR.sup.1, and a sulfinic acid or a salt thereof represented by the formulaR.sup.2 SO.sub.2 Y (II)wherein R.sup.2 is as defined above, and Y is a hydrogen atom, alkali metal atom, alkaline earth metal atom or quaternary ammonium are subjected to an electrolytic reaction in a mixture of water and an organic solvent in the presence of a halogen salt.
摘要翻译:本发明提供一种制备由式R 2 SO 2 S R 1(III)表示的硫代磺酸酯衍生物的方法,其中R 1为取代或未取代的2-苯并噻唑基,R 2为取代或未取代的苯基,该方法的特征在于式R1SX I)其中R1如上所定义,X是氢,碱金属或SR1,以及由式R2SO2Y(Ⅱ)表示的亚磺酸或其盐,其中R2如上定义,Y是氢原子,碱 金属原子,碱土金属原子或季铵在卤素盐存在下,在水和有机溶剂的混合物中进行电解反应。
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:
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 CN (VII)wherein R.sup.3 is defined above.
摘要:
The present invention provides a process for producing a .beta.-lactam halide compound represented by the general formula (2) which process is characterized in that the hydroxyl group of a .beta.-lactam halide compound represented by the general formula (1) is substituted with a halogen atom or a leaving group. ##STR1##
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.
摘要:
Disclosed is a method of producing a 3-exomethylenecepham of the formula ##STR1## wherein R.sup.1 is amino or substituted amino and R.sup.2 is a carboxy-protecting group comprising reacting a cephem of the formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined above and X is halogen with lead metal while maintaining the pH of the reaction system at about 0.1 to 8. The cephem (I) may be reacted with a catalytic amount of lead metal or a lead compound in the presence of a metal having a greater ionization tendency than lead.
摘要:
The present invention provides a process for preparing 3-norcephem compound represented by the formula (2), characterized in that a hydride reagent is acted on a halogenated .beta.-lactam compound represented by the formula (1) in the presence of a cuprous compound ##STR1## wherein R.sub.1 is a hydrogen atom, amino group or protected amino group, R.sub.2 is an aryl or substituted aryl, n is 0 to 2, R.sub.3 is a hydrogen atom or carboxylic acid protective group, X is a halogen atom, and Y is a halogen atom or a leaving group ##STR2## wherein R.sub.1 and R.sub.3 are as defined above.
摘要:
A process for preparing a .beta.-lactam derivative of formula (2) and/or the corresponding enol tautomer, which includes oxidizing an alkenyl-substituted .beta.-lactam derivative of formula (1) in the presence of a ruthenium catalyst or a rhenium catalyst using a periodic acid: ##STR1## wherein R.sup.1 is a hydrogen atom, a C.sub.1-4 alkyl group or a C.sub.1-4 haloalkyl group, R.sup.2 is a hydrogen atom, a C.sub.1-4 alkyl group or a phenyl group which may have a substituent, A is a group selected from ##STR2## wherein R.sup.3 is an amino group or a protected amino group, and R.sup.4 -R.sup.8 are as defined in the application.
摘要:
This invention provides a process for preparing 3-exomethylenecepham derivatives represented by the formula ##STR1## wherein R.sup.1 is arylacetylamino, aryloxyacetylamino, heterocyclic acetylamino or imido, and R.sup.2 is a protective group for the carboxyl, the process being characterized in that a 3-halomethylcephem compound represented by the formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, and X is a halogen atom is electrolyzed in a mixture of a hydrophilic organic solvent and water.
摘要:
The invention provides a process for preparing an allenyl .beta.-lactam of formula (4), by reacting the hydroxyl group of a .beta.-lactam of formula (1) with a reactive derivative of sulfonic acid of formula (2) to convert the compound of formula (1) to a .beta.-lactam of formula (3), thereafter reacting the resulting .beta.-lactam with a basic anion exchange resin of the type having a tertiary organic base fixed to the resin and isolating the allenyl .beta.-lactam of formula (4) with stability and high purity in a high yield.The invention also provides a process for preparing an allenyl .beta.-lactam of formula (4), by reacting the hydroxyl group of a .beta.-lactam compound of formula (1) with a reactive derivative of sulfonic acid of formula (2) to convert the compound of the formula (1) to a .beta.-lactam compound of formula (3), thereafter reacting the resulting .beta.-lactam of formula (3) with a tertiary organic base to convert the compound (3) to the allenyl .beta.-lactam of formula (4), thereafter causing two kinds of ion exchange resins, i.e., an acidic cation exchange resin and a basic anion exchange resin, to alternately or simultaneously act on the lactam of formula (4) and isolating the allenyl .beta.-lactam of formula (4).Further, the invention provides a process for preparing a 3-halogenated cephem of formula (6), characterized by causing a halogenating reagent to act on an allenyl .beta.-lactam of formula (4) in the presence of a sulfinate ion or thiolate ion capturing agent to obtain the 3-halogenated cephem.