| 摘要 |
PROBLEM TO BE SOLVED: To obtain a new compound comprising a specific acridine derivative, capable of manifesting an affinity for aδ-opiate receptor and useful as an analgesic agent. SOLUTION: This compound is represented by formula I R1 to R8 are as follows: R1 is A [A is a group represented by formula II (R11 is H or the like)] when R2 is H or the like; R3 is H or the like; R4 is CH2NR14R15 (R14 and R15 are each a 1-6C alkyl or the like); R5 and R6 are each H or the like and R7 and R8 are each H or the like; R9 and R10 are each H or the like; either one of X and Y is C and the other is N}, preferably rac-cis-[3- dimethylaminomethyl-2-(3-methoxy-phenyl)]-1,2,3,4-tetrahydro-acridin-2-ol hydrochloride, etc. The compound represented by formula I is obtained by reacting a compound represented by formula III (R19 is H or the like) or the like with a substituted 2-aminobenzaldehyde in the presence of an acid in a solvent such as a 1-4C alkyl alcohol, then reacting the resultant cyclization product with an acid and carrying out the elimination of the tertiary OH group or the separation of the methyl ether residue.
|
