PROCESS FOR THE PREPARATION OF 15-AMINO-20,21-DINOR-EBURNAMENINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

PCT No. PCT/FR89/00335 Sec. 371 Date Feb. 23, 1990 Sec. 102(e) Date Feb. 23, 1990 PCT Filed Jun. 28, 1989 PCT Pub. No. WO90/00171 PCT Pub. Date Jan. 11, 1990.A compound selected from the group consisting of a compound of the formula (I): in which R1 and R2 are individually selected from the group consisting of hydrogen, an alkyl of 1 to 5 carbon atoms, -(CH2)n-OH in which n is between 2 and 5, an aryl or arylalkyl of 7 to 12 carbon atoms, these two radicals being optionally substituted, in which R3 is an alkyl of 7 to 12 carbon atoms, these two radicals being optionally substituted, with the proviso that R1 and R2 are not both aryl simultaneously, or R1 and R2 form, together with the nitrogen atom to which they are linked, a saturated or unsaturated heterocyclic which can contain a second heteroatom chosen from oxygen, sulphur and nitrogen optionally substituted by an alkyl of 1 to 5 carbon atoms, aryl, arylalkyl of 7 to 12 carbon atoms, these radicals being optionally substituted, R4 and R5 are individually selected from the group consisting of hydrogen, halogen, alkyl or alkoxy of 1 to 5 carbon atoms, hydroxy, trifluoromethyl or nitro, the said products of formula (I) being in all the possible enantiomeric and diastereoisomeric forms and its non-toxic, pharmaceutically acceptable acid addition salts having an excellent analgesic activity.