PURPOSE: To obtain the title antibiotic of high purity extremely low in toxity in high yield by acylating an amino group of specific penicillanic acid by an acid halide in the presence of nicotin or the like.
CONSTITUTION: An amino group substd. at the 6-position of penicillanic acid wherein a carboxy group represented by formula I (wherein X is H or -OCOCH3) is protected (A) is acylated by an acid halide represented by formula II (wherein R is H or OH) (C) in the presence of a nicotin or isonicotine compd. as an acid receptor (B) to obtain the objective antibiotic represented by formula III. The acylation is pref. performed in the presence of compds. represented by formulae IV, V [wherein R1 is a group represented by formula VI or COOS (R2 and R3 are each H or 1-5C alkyl)].
MAROTTA VITTORIO (IT)
FARINA PAOLO (IT)
| JPS51149296A | 1976-12-22 | |||
| JPS5572194A | 1980-05-30 | |||
| JPS5069092A | 1975-06-09 |