Title:
6-METHOXY-1H-BENZOTRIAZOLE-5-CARBOXAMIDE DERIVATIVE AND MEDICINAL COMPOSITION CONTAINING THE SAME
Document Type and Number:
Japanese Patent JP3222051
Kind Code:
B2
Abstract:
PURPOSE: To obtain a new compound, having excellent antiemetic actions and hyperfunctions on alimentary canals and useful as an improving agent for functions of the alimentary canals due to weak central suppressing actions.
CONSTITUTION: This compound of formula I (R1 is ethyl or cyclopropylmethyl; R2 is H, methyl, etc.; (n) is 1-3; the wavy line indicates that the steric configuration of C atom to which the wavy line is bound is RS, R or S) or its salt, e.g. (R)-N-(1-ethyl-1H-hexahydroazepin-3-yl)-6-methoxy-1H-benzotriazole-5- carboxamide. The compound is obtained by reacting, e.g. a compound of formula II (R2a is R2 or an amino-protecting group) with a compound of formula III in the presence of a condensing agent such as N,N'-dicyclohexylcarbodiimide and a base such as NaOH at -10 to +150°C and then, as necessary, deprotecting the resultant compound. Furthermore, the compound of formula III is prepared by reacting, e.g. α-amino-ε-caprolactam with chlorotriphenylmethane, reducing the obtained reactional product and subsequently reacting the reduction product with a compound of the formula R1-X (X is a reactive ester residue of an alcohol).
Inventors:
Shiro Gato
Hirokawa Mimi
Hiroshi Yamazaki
Toshiya Morie
Naoyuki Yoshida
Hirokawa Mimi
Hiroshi Yamazaki
Toshiya Morie
Naoyuki Yoshida
Application Number:
JP32640295A
Publication Date:
October 22, 2001
Filing Date:
November 20, 1995
Export Citation:
Assignee:
Dainippon Pharmaceutical Co., Ltd.
International Classes:
C07D403/12; A61K31/41; A61K31/4192; A61K31/55; A61P1/00; A61P1/08; (IPC1-7): C07D403/12
Domestic Patent References:
| JP2104572A |
Attorney, Agent or Firm:
Hiroyuki Yoshioka