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Synthesis and antiarrhythmic activity of benzyl isoquinoline derivatives

Author: XiangYong
Tutor: XieMeiHua
School: Shanghai Institute of Pharmaceutical Industry
Course: Medicinal Chemistry
Keywords: Isoquinoline derivatives Antiarrhythmic Activity Benzyl Tetrahydroisoquinoline derivatives Alkyl benzene acetic acid Alkyl substituted Antiarrhythmic activity Antiarrhythmic drugs Amide derivative
CLC: R914
Type: Master's thesis
Year: 2000
Downloads: 153
Quote: 3
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Abstract


Find on ventricular tachycardia and ventricular fibrillation effective and safe anti-arrhythmic drugs , is an important direction for the study of cardiovascular drugs . In this paper, a class Ⅲ antiarrhythmic activity of benzyl isoquinoline derivatives SIPI - 926 as a lead compound , designed and synthesized a benzyl methylene mono-alkyl substituted 3,4 - dihydroisoquinoline quinoline derivative ( II ) , 1,2,3,4 - tetrahydroisoquinoline derivative ( III ) and the corresponding amide derivatives ( I ) . Synthesis of the target compounds , α- alkylphenyl acetic acid as raw materials , acid chloride , the and substituted phenethylamine condensation of the amide ( I ) , then by the Bischler-Napieralski reaction cyclization generated dihydroisoquinoline derivative ( II ) then sodium borohydride reduction the corresponding tetrahydroisoquinoline derivatives ( III ) . The key intermediate, α- alkylphenyl acetic acid was synthesized by the following four methods : (1) phenylacetonitrile α - alkylated , and then hydrolysis ; ( 2) phenyl - alkyl malonate hydrolysis decarboxylation ; (3) 2 - phenyl - 1 - nitrobutane hydrolysis; (4 ) phenylacetic acid , α -bit direct alkylation . Target compounds were characterized by elemental analysis , nuclear magnetic resonance , mass spectrometry confirmatory structure . \butylbenzyl ) -3,4 - dihydro- isoquinoline derivative ( II 6 < / sub >) , 1 - ( of α- ethyl- benzyl ) -1,2,3,4 - tetrahydro isoquinoline derivatives ( III 3 < / sub >) presented a dose-dependent prolongation of functional refractory period of activity , suggesting that it may have some anti-arrhythmic effects , but less active . The screening results show that the SIPI-926 of the lead compound , the methylene of the benzyl group of a monoalkyl-substituted , the antiarrhythmic activity decreased or disappeared .

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CLC: > Medicine, health > Pharmacy > Drug basic science > Medicinal Chemistry
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