Tricyclic compound and use thereof

摘要

The present invention relates to the compound represented by formula (I):;
(wherein, all the symbols have the same meaning as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.

主权项

1. A method of preparing a compound represented by formula (I-B-1-2): wherein R1 is a hydrogen atom, C1-8 alkyl, C1-8 alkoxy, or halogen atom and to is 0 or an integer of 1 to 4; R201 is selected from (1) methoxy which may have a fluorine atom(s), (2) isopropoxy which may have a fluorine atom(s), and (3) cyclopentyloxy which may have a fluorine atom(s); R202 is selected from (1) fluorine atom, (2) chlorine atom, (3) cyano, (4) methyl, and (5) methoxy which may have a fluorine atom(s) a salt thereof, an N-oxide thereof, or a solvate thereof the process comprising: (1) condensing an amine compound of the following formula (A):with a carboxylic acid of the following formula (B):in the presence of 1-hydroxy-7-azabensotriazole (HOAt) and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC), to obtain a compound of the following formula (C): (2) subjecting the compound of formula (C) to a cyclization reaction in the presence of phosphorous oxychloride to obtain a compound of the following formula (D): (3) Reducing the compound of the formula (D) in the presence of sodium borohydride to obtain a compound of the following formula (II)′: (4) subjecting the compound of the formula (II)′ to an amidation reaction in the presence of pyridine and acetic anhydride.