摘要:
A process for the production of a halogenated β-lactam compound represented by general formula (2) which comprises replacing the hydroxyl group of a halogenated β-lactam compound represented by general formula (1) with a halogen atom or a leaving group. Another process for the production of an exomethylene penam compound represented by general formula (5) which comprises reducing a halogenated β-lactam compound represented by general formula (2) with at least the equimolar amount of a metal having a standard oxidation-reduction potential of -0.3 (V/SCE) or below and 0.0001 to 10 times by mol as much a metal compound having a standard oxidation-reduction potential higher than that of the former metal, or employing the electrolytic reduction method.
摘要:
Taxane derivatives having a C13 side chain which includes an N-substituted group and the formula of the group is -COOX10 wherein X10 is alkyl, alkenyl or aryl. The taxane derivatives are useful antileukemia and anticancer agents.
摘要:
There is provided a process for preparing a compound of formula (I)
wherein R is H or a hydroxy protecting group, R₂ is an organic residue and R₃ is H or a nitrogen protecting group, which process comprises reacting together a compound of formula (II)
wherein R₁ is a C₁-C₄ alkyl or a phenyl group, R and R₃ are as defined above, a compound of formula (III)
wherein R₂ is as defined above and X is a cation or a silicon-containing residue, and a salt of a group IIa, IIb or transition element. The compounds of formula (I) are intermediates in the synthesis of penem antibiotics.
摘要:
A process for producing 3-[1′-(R)-hydroxyethyl]-4-acyloxyazetidinone from 3-[1′-(R)-hydroxyethyl]-4-alkyl (or aryl) thioazetidinone using a copper salt of aliphatic or aromatic carboxylic acid is disclosed. The process is an effective route for producing 3-[1′-(R)-hydroxyethyl]-4-acyloxyazetidinone, an intermediate for synthesizing penems or carbapenems, without using a mercury salt which can cause an environmental hazard.
摘要:
A process for preparing allenyl-β-lactam compounds of general formula (II) or 3-halocephem compounds of general formula (III) from halogenated β-lactam compounds of general formula (I) under reaction conditions selected depending on the objective compound. In formula (I), R1 is hydrogen, amino or protected amino; R2 is optionally substituted aryl; n is 0 to 2; R3 is hydrogen or a carboxyl-protecting group; X is halogeno; and Y is halogeno or a leaving group. In formula (II), R1, R2, n and R3 are each as defined above. In formula (III), R1, R3 and X are each as defined above.
摘要:
A process for producing a compound of the formula:
wherein R¹ represents a hydrogen atom or a hydroxy-protecting group, R² represents an organic group and R 3a represents a hydrogen atom or an acetoxymethyl group or a salt thereof, having a broad antibacterial spectrum and being of value as an antibacterial agent, and processes for producing intermediates used in the preparation of the compound (I) or a salt thereof, with remarkable industrial advantages.
摘要:
The present invention provides an allenyl β -lactam compound represented by the formula (1)
wherein R¹ is a hydrogen atom, halogen atom, amino or protected amino, R² is a hydrogen atom, halogen atom, lower alkoxyl, lower acyl, lower alkyl, lower alkyl substituted with hydroxyl or protected hydroxyl, hydroxyl or protected hydroxyl, R¹ and R² representing =O when taken together, R³ is a hydrogen atom or carboxylic acid protecting group, and X is the group -SO₂R⁴ or the group -SR⁴, R⁴ being substituted or unsubstituted aryl or substituted or unsubstituted nitrogen-containing aromatic heterocyclic group.