Tanabe Seiyaku Company, Limited

Ichizo Inoue

Yoshihisa Yamada

Toyonari Oine

Ryuichi Ishida

Kimiaki Hayashi

Takashi Ochiai

Yasuhiko Ozaki

Kenji Yamada

Hideyuki Takenaga

Kazuhiko Kondo

Junichi Tani

Takeshi Adachi

A thiophene derivative of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are a lower alkyl group, Ring A is a substituted or unsubstituted phenyl group and p is an integer of 1 to 3, or a salt thereof and processes for preparing the same are disclosed. The thiophene derivative (I) is useful as the regulator of gastrointestinal tract motility.

Thiophene derivative and process for preparing the same

A thiophen derivative of the formula: ##STR1## wherein R.sup.1, and R.sup.2 and R.sup.3 are a lower alkyl group, Ring A is phenyl, a lower alkylenedioxy-substituted phenyl, a phenyl group having 1 to 3 substituent(s) selected from the group consisting of a lower alkyl group, a lower alkylthio group, a lower alkoxy group, a phenyl-lower alkoxy group, a lower alkoxycarbonyl group, a halogen atom, amino group and hydroxy group, X is --OCO--, --O-- or --S--, m and n are an integer of zero or 1, and p and q are an integer of zero, 1 or 2, or a salt thereof.

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

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.

2-Fluoromethyl-3-o-tolyl-6-amino-4(3H)-quinazolinone

2,2'-Cyclocytidine is prepared by reacting cytidine with a functional derivative of silicon, and hydrolyzing the reaction product under acidic conditions. 1-.beta.-D-Arabinofuranosyl cytosine is prepared by reaction of cytidine with a functional derivative of silicon, followed by alkaline hydrolysis of the reaction product. 2,2'-Cyclocytidine and 1-.beta.-D-arabinofuranosyl cytosine are useful as antitumor and antiviral agents.

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Kawanishi, Japan

Ichizo Inoue