Toyama Chemical Co., Ltd.

Takashi Nagai

Isamu Saikawa

Takihiro Inaba

Hiroshi Sadaki

Isao Myokan

Hiroyuki Imaizumi

Yasuo Watanabe

Kenji Takeda

Shinzaburo Minami

Yoshikazu Fukuoka

Takako Hori

Hirokazu Ochiai

Shinji Miyabara

Hidetada Mikami

Masaaki Shibata

Nobuhisa Taya

Isao Myoukan

Keishi Funaki

Kenji Ohta

A novel isoindole derivative represented by general formula [1] or a salt thereof: ##STR1## which has an excellent antitumor activity and low toxicity.

Isoindole derivatives and salts thereof and antitumor agent comprising

This invention relates to a 7-amino-3-(pyrazinylmethyl)- or (pyridazinylmethyl)-cephalosporins of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents a group of the formula: ##STR2## in which R.sup.6 represents a hydrogen atom, a C.sub.1-5 alkyl group or a di-C.sub.1-5 alkylamino group; R.sup.13 represents a C.sub.1-5 alkyl group; and R.sup.28 represents an amino group.

7-amino-3-(pyrazinylmethyl) or (pyridazinylmethyl)-cephalosporins

The invention relates to antibiotic compounds of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents a group of the formula: ##STR2## R.sup.3 represents a hydrogen atom or an alkoxy group; R.sup.4 represents a hydrogen atom or a halogen atom; R.sup.5 represents a hydrogen atom or a protected or unprotected amino group; A represents a group of the formula, --CH.sub.2 -- or a group of the formula, ##STR3## or a group of the formula, ##STR4## and the bond  means that the compound may be a synisomer or an anti-isomer or a mixture thereof.

Antibiotic 7-(thiazolyl)-3-(pyrazinylmethyl) or (pyridazinylmethyl)

This invention relates to a novel process for producing a useful cephalosporin which comprises reacting a thiolo ester compound with a 7-aminocephalosporin in the presence of boron trifluoride or a complex compound thereof. This process enables the cephalosporin to be produced with a high purity in a high yield.

Novel process for producing cephalosporins

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Toyama, Japan

Takashi Nagai