METHOD OF SYNTHESIS OF 2,3-DIHYDRO-1,4-BENZOXAZINE DERIVATIVES IN THE FORM OF ISOMERS MIXTURE OR IN THE FORM OF INDIVIDUAL ISOMERS OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS

摘要

PCT No. PCT/EP89/00130 Sec. 371 Date Oct. 11, 1989 Sec. 102(e) Date Oct. 11, 1989 PCT Filed Feb. 13, 1989 PCT Pub. No. WO89/07596 PCT Pub. Date Aug. 24, 1989.The present invention relates to compounds having the following formula (I) (I) wherein X represents -O- or -S-; each of R and R1, independently, is hydrogen, halogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, amino, nitro or trihalo-C1-C6 alkyl; each of R2 and R3, independently, is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or phenyl-C1-C6 alkyl; or R2 and R3, taken together with the nitrogen atom to which they are linked, form an unsubstituted or substituted, 6-membered, saturated, heteromonocyclic ring optionally containing a further heteroatom chosen from oxygen, sulphur and nitrogen; each of R4 and R5, independently, is hydrogen, halogen, nitro, amino or trihalo-C1-C6 alkyl; and the pharmaceutically acceptable salts thereof. The compounds of the invention are useful in therapy as major tranquilizers e.g., in the management of psychotic disorders.