METHOD FOR ENZYMATIC SYNTHESIS OF (7S)-1-(3,4-DIMETHOXYBICYCLO [4.2.0]OCTA-1,3,5-TRIENE-7-YL)N-METHYL METHANAMINE AND APPLICATION THEREIN IVABRADINE SYNTHESIS
MOREAU, SANDRINE PEDRAGOSA,LEFOULON, FRANÇOIS,MORIS VARAS, FRANCISCO,MORIS VARAS, JAVIER
申请号:
GEAP2013013162
公开号:
GEP20156422B
申请日:
2013.07.15
申请国别(地区):
GE
年份:
2016
代理人:
摘要:
A method for synthesis of compound of for¬mula (IX), which value R1 is provided in the claims and, which is executed with enantioselective enzymatic acylation of racemic amine of formula (IV) with R1O-(CO)-OR1 carbonate by application of lipase dissolved in organic or water solvent or in their mix, at 25-40 °C tempe¬ra¬ture. Reduction of received compound of formula (IX) is executed by application of restorative agent: LiAlH4 or Red-Al, to produce compound of formula (I) applicable at ivabradine synthesis. Table: 5