Tanabe Seiyaku Company, Limited

Toyonari Oine

Yoshihisa Yamada

Totaro Yamaguchi

Satoshi Ohshima

Hiroshi Sugano

Mitsuyoshi Wagatsuma

Ryuichi Ishida

Ichizo Inoue

Takashi Ochiai

Masahiko Seto

Junichi Tani

Hironori Hayashi

Tadayuki Koumoto

Toshiya Kadowaki

There is disclosed a process for preparing 1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, or a salt thereof which comprises subjecting a propionate derivatives of the formula: ##STR2## wherein R.sup.2 is an ester residue and R.sup.1 is the same as defined above, to intramolecular cyclization in the presence of a sulfonic acid compound of the formula:

Process for preparing 1,5-benzothiazepine derivatives

Novel thiazolylacetic acid derivative of the formula: ##STR1## wherein R.sup.1.sub.N H-- is amino or a protected amino group, R.sup.2 is hydrogen or lower alkyl, --COOR.sup.3 is carboxy or a protected carboxy group and n is an integer of 2 or 3, and processes for preparing the same. The compound (I) is useful as an intermediate in the synthesis of cephalosporins.

Thiazolylacetic acid derivative and processes for preparing the same

A cephalosporin compound of the formula: ##STR1## wherein: R.sup.2 is a group of the formula: ##STR2## R.sup.4 is a lower alkenyl group, a lower alkyl group or a lower alkyl group substituted with a member selected from the group consisting of cyano, lower alkylthio, 2-(lower alkyl)-1,3,4-thiadiazol-5-yl, carbamoyl, thiocarbamoyl, and N-lower alkyl(thiocarbamoyl) and

Cephalosporin compounds

A cephalosporin compound of the formula: ##STR1## wherein R.sup.1 is a protected or unprotected amino group;

A cephalosporin compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl;

A quinazolinone derivative of the formula: ##STR1## wherein R is lower alkyl, lower alkoxy or halogen. Said quinazolinone derivative (I) or a pharmaceutically acceptable acid addition salt thereof is useful as central muscle relaxants.

Quinazolinone derivative

Thiazole intermediates for cephalosporin compounds

A 7.beta.-{(Z)-2-(2-aminothiazol-4-yl)-2-[(2-pyrrolidon-3-yl)oxyimino]acetam ido}-3-(1-amino-1H-tetrazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid or a pharmaceutically acceptable salt thereof is useful as an antimicrobial agent.

Pyrrolidomoxine cephalosporins

N-(2-amino-5-nitrobenzoyl)-o-toluidine is condensed with fluoroacetic acid or a functional derivative thereof. N-(2-fluoroacetamido-5-nitrobenzoyl)-o-toluidine obtained by said condensation reaction is dehydrated to produce 2-fluoromethyl-3-(o-tolyl)-6-nitro-4(3H)-quniazolinone, which is then subjected to reduction reaction. 2-fluoromethyl-3-(o-tolyl)-6-amino-4(3H)-quinazolinone thus obtained and a pharmaceutically acceptable acid addition salt thereof are useful as central muscle relaxants, minor tranquilizers, anti-convulsants, analgesics and/or anti-inflammatory agents.

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Nara, Japan

Toyonari Oine