| abstract |
REFERS TO A PROCEDURE FOR PREPARING 10,11-METHANOBENZOSUBERAN DERIVATIVES OF FORMULA I, WHERE: A IS -CH2-CH2-, -CH2-CHRa-CH2-, -CH2-CHRa-CH2-CH2; Ra IS OH; R1 AND R2 ARE H, F, Cl, Br; R3 IS HETEROARYL, PHENYL OPTIONALLY SUBSTITUTED WITH F, Cl, Br, CF3, CN, NO2, OCHF2 WHICH INCLUDES: a) REACTING A COMPOUND (4) WITH A SOURCE OF NUCLEOPHILES TO FORM A COMPOUND (5); b) REACTING A COMPOUND (5) WITH PIRAZINE TO FORM A COMPOUND (6); c) REDUCE THE COMPOUND (6) TO FORM A COMPOUND (8); d) REACTING A COMPOUND (8) WITH i) AN EPOXIDIC COMPOUND OF FORMULA (9) ii) A HALO COMPOUND OF FORMULA X1- (CH2) m-O-R3, X1 IS HALO, m IS 2-4; e) FORM A SALT OF THE COMPOUND (9) or (10). IT ALSO REFERS TO THE PREPARATION OF INTERMEDIATE COMPOUNDS. A PREFERRED COMPOUND IS (2R) -ANTI-5- TRICHLORHYDRATE {3- [4- (10,11-DIFLUOROMETHANODIBENZOSUBER-5-IL) PIPERAZIN-1-IL] -2-HYDROXYPROPOXI} QUINOLINE CRYSTALLINE HYDRATE, WHICH IT IS CHARACTERIZED BY ITS X-RAY DIFFRACTION PATTERN. THE COMPOUNDS MAY BE USEFUL FOR THE TREATMENT OF CANCER |