| 摘要 |
Synthesizing carbamate (IX) comprises performing an enantioselective enzymatic acylation of racemic form of (3,4-dimethoxy-7-bicyclo[4.2.0]octa-1,3,5-trienyl)methanamine (IV) with a lipase (EC 3.1.1.3 in the international classification of enzymes) by carbonate with 1-15 molar equivalents in organic solvents, aqueous solvents, a mixture of organic solvents and/or mixture of organic and aqueous solvents at a concentration of 5-500 g/l per liter of solvents and their mixtures, a E/S ratio of 10/1 to 1/100 and a temperature of 25-40[deg] C. Synthesizing carbamate of formula (IX) comprises performing an enantioselective enzymatic acylation of racemic form of (3,4-dimethoxy-7-bicyclo[4.2.0]octa-1,3,5-trienyl)methanamine of formula (IV) with a lipase (EC 3.1.1.3 in the international classification of enzymes) by carbonate of formula (R1O-(CO)-OR1) with 1-15 molar equivalents in organic solvents, aqueous solvents, a mixture of organic solvents and/or mixture of organic and aqueous solvents at a concentration of 5-500 g/l per liter of solvents and their mixtures, a E/S ratio of 10/1 to 1/100 and a temperature of 25-40[deg] C. R1 : linear or branched 1-6C-alkyl, allyl or benzyl. An independent claim is included for synthesis of (7S)-1-(3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-triene-7-yl) N-methyl methanamine of formula (I) comprising performing enzymatic acylation of (IV) to obtain (IX), and performing reduction step using a reducing agent consisting of lithium tetrahydridoaluminate and sodium bis(2-methoxyethoxy)aluminum hydride (Red-Al) to obtain (I). ACTIVITY : Cardiant; Vasotropic; Antianginal; Antiarrhythmic. MECHANISM OF ACTION : None given. |
