Patent · US Expired

Novel ampicillin esters and production thereof

US4389408A · kind A · utility

3Cited by
1References
9Claims
0Family size

Assignee

Inventors

Key dates

Filing dateDec 4, 1981
Grant dateJun 21, 1983
Priority date
Expiry dateDec 4, 2001

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D499/00
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A novel Ampicillin ester of the general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group or an aryl group, and R.sub.2 represents a hydrogen atom or may be taken together with R.sub.1 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-acylamino penicillanic acid (II) or its salt with a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, and X is a halogen atom, or reacting a compound of the formula ##STR3## wherein R.sub.1 and R.sub.2 are as defined above, or its acid addition salt with a corresponding carboxylic 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, deprotecting 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 and a method for the treatment of infectious disease.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.