Novel ampicillin esters and production thereof

专利名称：Novel ampicillin esters and production

thereof

发明人：Fumio Sakamoto,Shoji Ikeda,Goro

Tsukamoto,Isamu Utsumi

申请号：US06/327735申请日：19811204公开号：US04389408A公开日：19830621

摘要：A novel Ampicillin ester of the general formula ##STR1## wherein R.sub. 1represents a hydrogen atom, a methyl group or an aryl group, and R.sub. 2 represents ahydrogen atom or may be taken together with R.sub.1 to form a divalent carbon chainresidue, or its acid addition salt.

< P> The novel Ampicillin ester or its acid addition salt is prepared by (1) reacting acorresponding 6-N-acylamino penicillanic acid (II) or its salt with a compound of theformula ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, and X is a halogenatom, or reacting a compound of the formula ##STR3## wherein R. sub.1 and R.sub.2 areas defined above, or its acid addition salt with a corresponding carboxylic acid (VI) or itsreactive derivative, (2) thereafter, if required, when the resulting compound has theprotected amino group or the group convertible to an amino group, deprotecting theprotected amino group or converting said convertible group to an amino group, and (3) iffurther required, converting the product to an acid addition salt.< P>< P>The presentinvention provides also an antibacterial agent comprising the novel Ampicillin ester and amethod for the treatment of infectious disease.

申请人：KANEBO LTD.

代理机构：Wenderoth, Lind & Ponack

更多信息请下载全文后查看