Dissertation > Medicine, health > Pharmacy > Drug basic science > Medicinal Chemistry

Synthesis of calcium sensitizer levosimendan

Author ChenGuiRong
Tutor ChenYuBin
School Shenyang Pharmaceutical University
Course Medicinal Chemistry
Keywords Levosimendan Heart Failure Calcium sensitizer Synthesis Medicinal Chemistry
CLC R914
Type Master's thesis
Year 2006
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This article briefly the pathogenesis of heart failure and drug treatment , described in detail the mechanism of its development overview of the role of the anti-heart failure drug , levosimendan . In reference to the literature on the basis of L-lactic acid as the starting material by esterification , replaced by acid hydrolysis , the Friedel-Crafts acylation , alkylation , hydrolysis , catalytic hydrogenolysis , cyclization and diazotization 12 of step reaction of levosimendan , and its structure was confirmed by mass spectrometry , NMR conclusive evidence of the total yield increased by 0.5 % compared to literature . Meanwhile, 4 , 6 , 8 and 9, the reaction conditions of levosimendan and its important intermediates more detailed research and study , in which 6.5 % Synthesis of Intermediate 4 in yield compared with the literature ; Intermediate 8 the increase in yield compared with literature ; in the intermediates 6 synthesis using cheap nitrobenzene instead of the literature relatively expensive 1,2,4 - trichlorobenzene , 1% increase in yield than reported in the literature , the cost significantly reduced; with inexpensive readily available sodium methoxide instead of sodium hydride, to simplify the operating conditions reported in the literature during the synthesis of the intermediate 9 . Furthermore, in the intermediate 2,6,7 and 11 post-treatment process using recrystallization instead of column chromatography method reported in the literature , to shorten the cycle of operation , simplifies the experimental procedures , reduce production costs and facilitates in large The scale used in the production .

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