- 1,1-Alkanediol dicarboxylate linked antibacterial agents
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Useful antibacterial agents in which a penicillin and/or a beta-lactamase inhibitor are linked via 1,1-alkanediol dicarboxylates are of the formula STR1 where A is the residue of certain dicarboxyic acids, R3 is H or (C1 -C3), n is zero or 1 such that when n is zero R is P or B and R1 is the residue of certain esters, H or a salt thereof; and when n is 1, one of R and R1 is P and the other is B, and P is STR2 where R2 is H or certain acyl groups, and B is the residue of a beta-lactamase inhibiting carboxylic acid; a method for their use, pharmaceutical compositions thereof and intermediates useful in their production.
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- Bis-esters of dicarboxylic acids with amoxicillin and certain hydroxymethylpenicillanate 1,1-dioxides
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Antibacterial bis-esters of 1,4-cyclohexanedicarboxylic acids and alkane dicarboxylic acids wherein the ester moieties are derived from different alcohols; one alcohol being hydroxymethylpenicillanate 1,1-dioxide, or the 6-beta-hydroxymethyl or the 6-alpha-aminomethyl derivative thereof; and the other being 6-[D-(2-amino-2-(p-hydroxyphenyl)acetamido)]penicillanic acid (amoxicillin); and pharmaceutically acceptable salts thereof; a method for the use of said esters and their salts, and methods for their preparation.
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- Geminate-Substituted Cyclopentadienes. 1. Synthesis of 5,5-Dialkylcyclopentadienes via 4,4-Dialkylcyclopent-2-en-1-ones.
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A synthetic route for the preparation of 5,5,-dialkylcyclopentadienes (1) via 4,4-dialkylcyclopent-2-en-1-ones (3) is described.Beginnig with ketones (in which the two carbonyl substituents will become the two alkyl groups in the title compounds), the route traverses the Guareschi imides 5, 3,3-dialkylglutaric acids 4 and their ethyl esters 7, masked acyloins 8, cyclopentenones 3, alkohols 9, and bromides 10 to reach the dienes 1.Physical properties of five such derivates 1 and 3 (dimethyl, methylethyl,diethyl, methyl-n-propyl, and methylisopropyl) are presented.
- Holder, Richard W.,Daub, John P.,Baker, Wesley E.,Gilbert, Raymond H,Graf, Norman A.
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p. 1445 - 1451
(2007/10/02)
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