Enzymatic synthesis procedure of (7S) -1- (3,4-dimethoxybicyclo 4.2.0 octa-1,3,5-trien-7-yl) N-methylmethanoamine and its use in the synthesis of ivabradine and its you go out

摘要

Synthesis procedure of the compound of formula (IX): ** Formula ** where R 1 represents a linear or branched (C 1 -C 6) alkyl group, allyl or benzyl, by enantioselective enzymatic acylation of the racemic amine of formula (IV): ** Formula ** with the help of a lipase (EC 3.1.1.3 in the international classification of enzymes): with a carbonate of formula R1O- (CO) -OR1 where R1 has the meaning defined above, in an amount that has from 1 to 15 molar equivalents with respect to the amine of formula (IV), in an organic, aqueous solvent, a mixture of organic solvents or a mixture of organic and aqueous solvents, at a concentration of 5 to 500 g / l of the compound of formula (IV ) per liter of solvent or solvent mixture, in an I / O ratio of 10/1 to 1/100, at a temperature of 25ºC to 40ºC.