| Landiolol Hydrochloride is a new type of higher selectivity β1-adrenergic receptor blocking agent, Its named as (2,2-dimethyl-1,3-dioxolan-4S-yl) methyl-3-{4-[2S-hydroxy-3-(2-morpho linocarbonyl amino) ethylamino] proxy] phenyl} propinate hydrochloride. It was used in emergency treatment of tachycardia and better control of heart rate in surgery, which possesses higher β1-selectivity, ultra short-acting, short elimination half-life, lower toxic and less side effect.The paper have redesigned the way of synthesize landiolol hydrochloride through contrasted some ways which come from reference.(2,2-dimethyl-1,3-dioxolan-4S-yl)methyl-3-[4-(2,3-epoxypropox)phyen-yl]propionate was synthesized simply and efficiently from S(+)-epichlorohydrin through condensation reaction, esterification reaction, etherification reaction. In the same time we have optimize the operations in the process of experimentation. The intermediate2-(morpholino-carbonylamino) ethylamine oxalic acid was synthesized, from added morphpline, ethylenediamine and oxalic acid to N,N’-carbonyl-diimidazole, reaction at room temperament. Then.2-(morpholino-carbonylamino)ethylamine oxalic acid resolved and reacted with (2,2-dimethyl-1,3-dioxolan-4S-yl) methyl-3-[4-(2,3-epoxy-propox) phyenyl]propionate, reaction in the mixed system of water and isopropanol. Obtainmented (2,2-dimethyl-1,3-dioxolan-4S-yl) methyl-3-{4-[2S-hydroxy-3-(2-morpholinocarbonylaminoethyl-)aminopropoxyl]ph yenyl}propionate.At last gained its hydrochloric viz.landiolol hydro-chloride.In the process of experiment, we optimize the route of synthesize landiolol hydrochloride, predigest the experiment operation, make the way fit volume-produce and industrialisation-produce. In the same time, the structure of intermediate was identified with infrared spctra, magnetic resonance, electrospray ionization mass spectra and the others way. All of them were confirmed, and final-produce confirmed by DEPT135, HMBC and HSQC, the planar-magnetic resonance. |
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