| 摘要 |
1315630 Penicillins BEECHAM GROUP Ltd 21 March 1972 [31 March 1971] 8754/71 Heading C2A The invention comprises a penicillin of Formula II or a salt or an ester thereof, wherein X represents [-O-], [-S-], a grouping of Formula III or wherein R is hydrogen, alkyl or aralkyl and a and b are each integers such that a + b = 4. Such penicillins include 6-[4-amino-1-thiacyclohexan - 4 - yl - carbamido] - penicillanic acid, 6 - [4 - aminotetrahydropyran - 4 - yl - carbamido]-pencillanic acid, 6-[3-amino-1-thiacyclohexan-3-yl-carbamido penicillanic acid, 6-[4- amino - 1,1 - dioxo - 1 - thiacyclohexan - 4 - ylcarbamido] - penicillanic acid, 6 - [4 - amino - 1- benzylpiperid-4-yl-carbamido]-penicillanic acid and salts and esters thereof. A process for the preparation of compounds of Formula II comprises reacting 6-aminopenicillanic acid or a salt or ester thereof, or silyl 6-amino penicillanic acid with a reactive N-acylating derivative of an acid of Formula IV wherein X, a and b are as previously defined and Y is a nitrogen-containing group which may be converted into a primary amino group, and subsequently converting the group Y into a primary amino group. |
