Ampicillin esters and production thereof

C - Chemistry – Metallurgy – 07 – D

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260/114.7

C07D 499/42 (2006.01) C07D 317/40 (2006.01) C07D 317/64 (2006.01) C07D 499/00 (2006.01) C07D 499/68 (2006.01)

Patent

CA 1212105

- 1 - Title of Invention NOVEL AMPICILLIN ESTER AND PRODUCTION THEREOF Abstract of Disclosure A novel Ampicillin ester of the general formula Image wherein R1 represents a hydrogen atom, a methyl group or an aryl group, and R2 represents a hydrogen atom or may be taken together with R1 to form a divalent carbon chain residue, or its acid addition salt. The novel Ampicillin ester or its acid addition salt is prepared by (1) reacting a corresponding 6-N-acyl- amino penicillanic acid (II) or its salt with a compound of the formula Image .....(III) wherein R1 and R2 are as defined above, and X is a halogen atom, or reacting a compound of the formula Image .....(V) wherein R1 and R2 are as defined above, or its acid addition salt with a corresponding carboxylic - 2 - acid (VI) or its reactive derivative, (2) thereafter, if required, when the resulting compound has the protected amino group or the group convertible to an amino group, de- protecting the protected amino group or converting said convertible group to an amino group, and (3) if further required, converting the product to an acid addition salt. The present invention provides also an antibacterial agent comprising the novel Ampicillin ester.

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