Synthesis of morphinans with reduced herg activity and mop binding

A compound according to general formula (I)

• wherein
• R1 means —H, —OH, —CO2H, —R0, —OR0, —OC(═O)R0, —OC(═O)OR0 or —OC(═O)NHR0;
• R2 means —H, —R0, —C(═O)R0, —C(═O)OR0 or —C(═O)NHR0;
• X means —SR0 or —NR3R4, wherein
• R3 means —H, —R0, —C(═O)R0, —C(═O)OR0, —C(═O)NHR0, —C(═O)N(R0)2, —C(═O)NH2, —C(═O)CH(NH2)R0 or —S(═O)2R0;
• and R4 means —C(═O)R0, —C(═O)OR0, —C(═O)NHR0, —C(═O)N(R0)2, —C(═O)NH2, —C(═O)CH(NH2)R0 or —S(═O)2R0;
• or
• R3 and R4 together with the nitrogen atom to which they are attached form an azetidine ring, a pyrrolidine ring, a piperidine ring, a piperazine ring, a pyrazole ring, a triazole ring, an imidazole ring, or a spirocyclic compound containing an azetidine ring and an oxetanyl ring, in each case independently unsubstituted or substituted with one or two substituents independently selected from the group consisting of ═O, —F, —CH3, —C(═O)NH2, —C(═O)NHCH3, —SO2CH3, —NH2 and —N(CH3)2;
• wherein R0 in each case means -C1-6-alkyl, -C3-12-cycloalkyl, -C1-6-alkylene-C3-12-cycloalkyl, -C3-12-heterocycloalkyl, -C1-6-alkylene-C3-12-heterocycloalkyl, -C6-14-aryl, -C1-6-alkylene-C3-6-aryl, -C3-14-heteroaryl or —C1-6-alkylene-C3-14-heteroaryl, in each case independently unsubstituted or substituted;
• wherein in each case -C1-6-alkyl may be linear or branched, saturated or unsaturated, unsubstituted or substituted;
• wherein in each case -C1-6-alkylene- may be linear or branched, saturated or unsaturated, unsubstituted or substituted;
• wherein in each case -C3-12-cycloalkyl may be saturated or unsaturated, unsubstituted or substituted;
• wherein in each case -C3-12-heterocycloalkyl may be may be saturated or unsaturated, unsubstituted or substituted;
• wherein in each case -C6-14-aryl may be unsubstituted or substituted;
• wherein in each case -C3-14-heteroaryl may be unsubstituted or substituted;
• wherein in each case “substituted” means mono- or polysubstituted with one or more substituents independently of one another selected from -C1-6-alkyl, —F, —Cl, —Br, —I, and —NH2;
• or a physiologically acceptable salt thereof.