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US 7,553,989 B2Granted
Malonic acid monoesters and process for producing the same
AssigneeMeiji Seika Kaisha, Ltd.
InventorsTakehiko Sawabe, Kazuhiro Aihara, Kunio Atsumi, Keiichi Ajito
Life of this patent
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Abstract
The present invention relates to a compound represented by formula (1) or a salt thereof: wherein R represents a group that is easily removable upon hydrolysis in vivo. This compound is usable in the production of prodrug-type carbapenem antibacterial agents for oral administration. The use of this compound in the process of production of the antibacterial agents can realize enhanced production efficiency and reduced production cost.
Claims2
A compound represented by formula (1) or a salt thereof:
- wherein R represents
- (a) C1-C6 alkylcarbonyloxy C1-C2 alkyl optionally substituted by cyclohexyl,
- (b) phenylcarbonyloxy C1-C2 alkyl in which the phenyl part is optionally substituted by C1-C4 alkyl,
- (c) C1-C6 alkoxycarbonyloxy C1-C2 alkyl optionally substituted by cyclohexyl,
- (d) phenyloxycarbonyloxy C1-C2 alkyl in which the phenyl part is optionally substituted by C1-C4 alkyl,
- (e) unsubstituted C3-C6 cycloalkyloxycarbonyloxy C1-C2 alkyl, or
- (f) unsubstituted 2-oxo-5-(C1-C4 alkyl)-1,3-dioxolen-4-ylmethyl.
4 more elements
A compound selected from the group consisting of:
- monoacetyloxymethyl malonate,
- monopivaloyloxymethyl malonate,
- mono-2,4-dimethylbenzoyloxymethyl malonate,
- mono-1-(ethoxycarbonyloxy)ethyl malonate,
- mono-1-(isopropoxycarbonyloxy)ethyl malonate,
- monocyclohexyloxycarbonyloxymethyl malonate,
- mono-1-(cyclohexyloxycarbonyloxy)ethyl malonate,
- mono-1-(phenoxycarbonyloxy)ethyl malonate,
- mono-2-oxo-5-methyl-1,3-dioxolen-4-ylmethyl malonate,
- mono-1-(2,2-dimethylpropoxycarbonyloxy)ethyl malonate,
- mono-1-(2-cyclohexylethoxycarbonyloxy)ethyl malonate,
- mono-1-(isobutoxycarbonyloxy)ethyl malonate,
- monoisopropoxycarbonyloxymethyl malonate,
- monoisopentoxycarbonyloxymethyl malonate,
- monoisobutylcarbonyloxymethyl malonate, and
- mono-1-ethylpropylcarbonyloxymethyl malonate.
13 more elements
Dependencies are inferred from the claim text.