摘要:
A process for producing a 3-substituted cephem compound from an allenyl-β-lactam compound which can readily be prepared from an inexpensive penicillin compound in a short reaction path. The process comprises reacting an allenyl-β-lactam compound with an organohalogen compound in the presence of an at least equimolar amount of a metal having a standard oxidation-reduction potential of -0.3 V/SCE or less and 0.0001 - 0.5 mol, per mole of the lactam, of a metallic compound having a standard oxidation-reduction potential higher than that of the above metal.
摘要:
A β-lactam compound and a 2-(substituted methyl)-3-cephem compound, both being useful as an intermediate for the synthesis of cephem antibiotics and so forth. The lactam compound is represented by general formula (I), wherein R¹ represents protected amino, etc.; R² represents hydrogen, etc.; R³ represents hydrogen or a protective group for a carboxyl group; R⁴ represents optionally substituted aryl; and R⁵ represents optionally substituted alkenyl, etc. The cephem compound is represented by general formula (II), wherein R¹, R² and R³ are each as defined above; and R⁶ represents optionally substituted aryl.
摘要翻译:β-内酰胺化合物和2-(取代的甲基)-3-头孢烯化合物都可用作合成头孢烯抗生素等的中间体。 内酰胺化合物由通式(I)表示,其中R 1表示被保护的氨基等; R 2表示氢等; R 3表示氢或羧基的保护基; R 4表示任选取代的芳基; 并且R 5表示任选取代的烯基等。头孢烯化合物由通式(II)表示,其中R 1,R 2和R 3各自如上所定义; 且R 6表示任选取代的芳基。
摘要:
Cephalosporin compounds represented by general formula (I), pharmacologically acceptable addition salts thereof, method for the production thereof, and medicinal uses thereof, wherein R1 represents hydrogen or lower alkyl, and R2 represents 1-alkanoyloxyalkyl or 1-alkoxycarbonyloxy-alkyl. These compounds and salts not only can be readily absorbed through the digestive tract to exhibit wide antibacterial activities in vivo in the form of the hydrolyzates thereof, but also have remarkable sweetness 10 to 400 times as high as that of sucrose. Therefore they are useful in preventing and treating infectious diseases by oral administration.
摘要:
The present invention relates to new cephalosporins of the formula
wherein R¹ and R² are hydrogen or carboxy, with the proviso that both cannot be the same; R³ is hydrogen or acetyl; and R⁴ is a radical selected from the group consisting of
or -CH=CH-CH₂-R⁶ in which n is 1 or 2, R⁵ is hydrogen or acetyl, and R⁶ is hydrogen, a lower C₁₋₃ alkyl, or a radical selected from the group consisting of
in which n and R⁵ are as defined above. In another aspect, this invention relates to processes for the preparation of the compounds of Formula I, to pharmaceutical compositions containing at least one compound of Formula I, and to intermediates in their preparation.
摘要:
3-Fluorosulfonyloxyceph-3-ems having a protected amino or acylamino group in the 7-position are subject to carbon-carbon bond formation at the 3-position by means of a palladium catalyzed coupling reaction with substituted organostannanes. A process for preparing cefprozil is disclosed.
摘要:
As new antibacterial compounds are provided a cephalosporin derivative having the general formula (I) wherein R¹ is a lower alkyl group, a lower alkoxymethyl group or a lower alkenyl group, and R² and R³ are each a hydrogen atom or a lower alkyl group, and pharmaceutically acceptable salt thereof. This new cephalosporin derivative of the formula (I) is useful as an orally administrable antibacterial agent which exhibits an excellent antibacterial activity, high absorbability through the digestive tracts of animal and high urinary recovery thereof.