Toyama Chemical Co., Ltd.

Hirohiko Fukuda

Yoshiharu Murotani

Isamu Saikawa

Shuntaro Takano

Kaishu Momonoi

Hiroyuki Imaizumi

Takihiro Inaba

Yasuo Watanabe

Ryuko Takeno

Kiyoshi Tanaka

Hirokazu Ochiai

Shinzaburo Minami

Seishi Morita

Osamu Yoshino

Toshio Hayashi

Junichi Yoshida

A penam derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom, an amino-protecting group or an acyl group; R.sup.2 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a lower alkoxy group, a lower alkylthio group or a formamido group; R.sup.4 represents an protected or unprotected carboxyl group or a carboxylato group; R represents a group of the formula, --NHR.sup.5 or --NR.sup.5 R.sup.6 (in which R.sup.5 and R.sup.6, which may be the same or different, represent protected or unprotected hydroxyl groups, cyano groups, sulfo groups, or unsubstituted or substituted lower alkyl, aryl, acyl, carbamoyl, sulfamoyl, lower alkylsulfonyl or heterocyclic groups) or a group of the formula, --N.dbd.CR.sup.7 R.sup.8 (in which R.sup.7 and R.sup.8, which may be the same or different, represent hydrogen atoms or protected or unprotected carboxyl groups, cyano groups or unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl, aryl, amino, acyl, acyloxy, carbamoyl, carbamoyloxy, sulfamoyl, lower alkylthio, ureido or heterocyclic groups, or R.sup.7 and R.sup.8 may form a cycloalkene or a heterocyclic ring with the carbon atom to which R.sup.7 and R.sup.8 are attached); and n represents 1 or 2. The above penam derivative or its salt is very effective as antibacterial agents.

Penam derivatives and salts thereof, process for producing the same and

A penam derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom, an amino-protecting group or an acyl group; R.sup.2 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a lower alkoxy group, a lower alkylthio group or a formamido group; R.sup.4 represents a protected or unprotected carboxy group or a craboxylato group; R represents a group of the formula, --NHR.sup.5 or --NR.sup.5 R.sup.6 (in which R.sup.5 and R.sup.6, which may be the same or different, represent protected or unprotected hydroxyl groups, cyano groups, sulfo groups, or unsubstituted or substituted lower alkyl, aryl, acyl, carbamoyl, sulfamoyl, lower alkylsulfonyl or heterocyclic groups) or a group of the formula, --N.dbd.CR.sup.7 R.sup.8 (in which R.sup.7 and R.sup.8, which may be the same or different, represent hydrogen atoms or protected or unprotected carboxyl groups, cyano groups or unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl, aryl, amino, acyl, acyloxy, carbamoyl, carbamoyloxy, sulfamoyl, lower alkylthio, ureido or heterocyclic groups, or R.sup.7 and R.sup.8 may form a cycloalkene or a heterocyclic ring with the carbon atom to which R.sup.7 and R.sup.8 are attached); and n represents 1 or 2. The above penam derivative or its salt is very effective as antibacterial agents.

Penam derivatives and salts thereof, and antibacterial agent comprising

The invention relates to a process for producing a cephalosporin of the formula ##STR1## by reacting the compound ##STR2## with the compound ##STR3## in the presence of boron trifluoride or a complex thereof.

Novel process for producing a cephalosporin

This invention relates to a novel aminothiazole intermediate for production of a cephalosporin of antibiotic activity.

Aminothiazole intermediate for a cephalosporin

Growing community of inventors

Toyama, Japan

Hirohiko Fukuda