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    • 9. 发明授权
    • Novel ampicillin esters and production thereof
    • 新型氨苄西林酯及其生产
    • US4389408A
    • 1983-06-21
    • US327735
    • 1981-12-04
    • Fumio SakamotoShoji IkedaGoro TsukamotoIsamu Utsumi
    • Fumio SakamotoShoji IkedaGoro TsukamotoIsamu Utsumi
    • C07D317/40C07D317/64C07D499/00C07D499/12C07D499/32C07D499/42C07D499/68A61K31/43
    • C07D317/40C07D317/64C07D499/00
    • 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.
    • 一种通式为“IMAGE”的新型氨苄青霉素酯,其中R 1表示氢原子,甲基或芳基,R 2表示氢原子,或可与R 1一起形成二价碳链残基,或其酸 加盐。 通过(1)使相应的6-N-酰基氨基青霉烷酸(II)或其盐与式(III)的化合物反应,其中R 1和R 2如上所定义,制备新型氨苄青霉素酯或其酸加成盐 或者其中R1和R2如上所定义的式(VI)化合物或其酸加成盐与相应的羧酸(Ⅵ)或其反应性衍生物反应, 2)此后,如果需要,当所得化合物具有被保护的氨基或可转化为氨基的基团时,将保护的氨基脱保护或将所述可转换基团转化为氨基,和(3)如果需要,将 产物加酸加成盐。 本发明还提供了包含新型氨苄青霉素酯的抗菌剂和治疗感染性疾病的方法。