METHOD OF SYNTHESISING DERIVATIVES OF AMINO-METHYL TETRALIN Russian patent published in 2014 - IPC C07C231/06 C07C231/12 C07C231/16 C07C317/32 

FIELD: chemistry.

SUBSTANCE: invention relates to method of obtaining formula k1 or k2 compound, where m has value 0 or 1; n has value from 0 to 3; Ar represents aryl or heteroaryl, each of which can be possibly substituted and have as substituents: halogeno, C_1-6alkyl, C_1-6alcoxy, cyano, hydroxy, C_1-6alkylsulfonyl or halogeno-C_1-6alkyl; Y represents -O-; -S(O)_p- or -N-R^a, where p has value from 0 to 2 and R^a represents hydrogen atom or C_1-6alkyl; and R¹ represents halogeno, C_1-6alkyl, C_1-6alcoxy or halogeno-C_1-6alkyl. Method is realized by reduction of dihydronaphthalene amide of formula i with gaseous hydrogen in presence of ruthenium catalyst or where D represents possibly chiral diamine, each of E and E' represents halogeno, or E represents hydrogen atom and E' represents BH₄; L represents chiral diphosphine ligand; Z represents halogeno or R^b-CO₂- (carboxylate), where R^b represents: C_1-6alkyl, halogeno-C_1-6alkyl, C_1-6alcoxy, aryl, possibly having halogen atom as substituents, or heteroaryl, possibly having halogen atom as substituents. By reduction of k1 and k2 compounds it is possible to obtain respective compounds of formulas m1 and m2 , which in case of interaction with reagent of formula X-R², where X represents leaving group; R² represents -C(O)-R^c or -SO₂-R^c, where R^c represents C_1-6alkyl or -NR^dR^e, each of R^d and R^e independently represents hydrogen atom or C_1-6alkyl, result in obtaining formula o1 and o2 compounds.

EFFECT: improved method of obtaining tetralin derivatives.

35 cl, 6 dwg, 7 tbl, 10 ex