摘要:
A process for photochemically converting 3-exomethylene cephams (or 1-carba(1-dethia)cephams or 1-oxa(1-dethia)cephams) from the corresponding 3-alkyl-3-cephem (or 1-carba(1-dethia)cephem or 1-oxa(1-dethia)cephem) is provided. Further provided are 3-cephams useful as intermediates to 3-cephem compounds.
摘要:
A process for photochemically converting 3-exomethylene cephams (or 1-carba(1-dethia)cephams or 1-oxa(1-dethia)cephams) from the corresponding 3-alkyl-3-cephem (or 1-carba(1-dethia)cephem or 1-oxa(1-dethia)cephem) is provided. Further provided are 3-cephams useful as intermediates to 3-cephem compounds.
摘要:
The crystalline dihydrate and trihydrate forms of the antibiotic 7β-[2′-(R)-2′-phenyl-2′-aminoacetamido]-3-chloro-3-(1-carbadethiacephem)-4-carboxylic acid ("LY163892") are described. These hydrates are antibiotics in their own right, and are valuable intermediates to the corresponding monohydrate form of LY163892.
摘要:
The invention provides a free radical process for preparing 1-carba(1-dethia)cephalosporin antibiotics with 2-substituted methylcephalosporin 1,1-dioxides wherein the substituent on the 2-methylene group is a free radical precursor group such as a phenyl or alkylseleno group. The latter dioxides are treated with a free radical initiator, e.g., a trialkyltin hydride or actinic radiation at 40°C to 150°C to provide the 1-carba-3-cephem and 1-carba-2-cephem products. The invention also provides free radical compounds formed as intermediates in the process.
摘要:
Nouveau compose ayant un noyau contenant un systeme (Beta)-lactame carbocyclique benzoique. Le compose a une action antibacterienne contre le B. subtilis.
摘要:
An industrially excellent novel process for the preparation of addition salts of basic antibiotics with inorganic acids (such as hydrochloric acid), by subjecting a basic antibiotic-oxalic acid addition salt (II) to salt-exchange with an inorganic acid salt (III) of an alkaline earth metal, wherein A is a basic antibiotic; R10 is a protected functional group to be used in organic synthesis; Ak-E is an alkaline earth metal; and B is an inorganic acid; carbapenem derivative-oxalic acid addition salts represented by general formula (II-I) and being useful as intermediates for the preparation of hydrochlorides of antimicrobial agents; and a process for preparing the same, (II-I) wherein A is a three- to seven-membered ring having at least one nitrogen atom; R1 is hydrogen or the like; R?2 and R5¿ are each hydrogen or a protecting group; R3 is a protecting group; R4 is hydrogen or the like; and R6 is hydrogen or the like.
摘要:
The invention provides new fluorinated cephalosporin antibiotics of Formula I wherein
R a , R b , R c , R d and R e , independently, are H, F or C 1 -C 6 alkyl-(Z) n - group having at least one fluorine substituent; X is O or S; Y is S, O, or -CH 2 -; Z is O, S, -SO-, or -SO 2 -; m and n independently are 0 or 1; and R 1 is H, C 1 -C 6 -alkyl, phenyl or benzyl, each of which may optionally have up to three substituents selected from halo, C 1 -C 4 -alkoxy, phenyl, NO 2 , C 1 -C 6 -alkanoyl, benzoyl, or C 1 -C 6 -alkanoyloxy; or a physiologically acceptable salt thereof; provided that:
1) at least one of R a , R b , R c , R d or R e is other than hydrogen; and 2) when R e is F, or one of R b or R d is CF, at least one of the remaining R a , R b , R c , R d or R e is other than hydrogen, processes for preparing these compounds and veterinary and pharmaceutical formulations containing a Formula I compound as an active ingredient.