C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 319/20 (2006.01) C07C 255/32 (2006.01)
Patent
CA 2102109
2102109 9221671 PCTABS00017 New N-Arylalkylderivatives of 2-aminomethyl-2,3-dihydro-1,4-benzodioxine and its (+)- and (-)-enantiomers represented by general formula (I), where R1, R2 and R3 represent H, or R1 and R2 represent H and R3 represent methyl, or R1 and R2 represent methoxy and R3 represents H and their pharmaceutically acceptable organic or inorganic acid addition salts exhibit in pharmacological tests pronounced hypotensive activity as a result of their calcium channel blocking and alpha1-adrenergic blocking activity and pronounced antithrombotic action. In a form of pharmaceutical preparations, they are suitable for the treatment and prevention of cardiovascular diseases and other disorders. New compounds of general formula (I) by N-alkylation of 2-aminomethyl-2,3-dihydro-1,4-benzodioxine and its (+)- and (-)-enantiomers by derivatives of 2-phenyl-2-isopropyl-5-oxovaleronitrile under the conditions of reductive alkylation or with derivatives of 5-bromo-2-phenyl-2-isopropylvaleronitrile, which can be prepared by allylation of alpha-isopropylbenzyl cyanide and subsequent addition of hydrogen bromide under free radical conditions to the obtained alpha-allyl-alpha-isopropylbenzyl cyanide and its derivatives.
Butora Gabriel
Helfert Ivan
Rajsner Miroslav
Trcka Vaclav
Gowling Lafleur Henderson Llp
Vyzkumny Ustav Pro Farmacii A. Biochemii S.p.
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