- NOVEL PROCESS FOR THE PREPARATION OF GADOLINIUM COMPLEX OF (4S)-4-(4-ETHOXYBENZYL)-3,6,9-TRIS(CARBOXYLATOMETHYL)-3,6,9- TRIAZAUNDECANEDIOIC ACID DISODIUM (GADOXETATE DISODIUM)
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The present invention discloses a novel process for the preparation of gadolinium complex of (4S)-4-(4-Ethoxybenzyl)-3,6,9-tris(carboxylatomethyl)-3,6,9- triazaundecanedioic acid disodium of formula 1 and novel intermediates thereof.
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- A S-1 - (4- ethoxy group phenmethyl ) - 3-aza-pentane -1,5- diamidogen three hydrochloride preparation method
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The invention relates to a preparation method of S-1-(4-ethyoxylbenzyl)-3-azapentane-1,5-diaminetrihydrochloride. The preparation method comprises the following steps: adopting L-tyrosine alkyl ester as a starting raw material, carrying out alkylation reaction with bromoethane, carrying out reduction on an obtained product by use of sodium borohydride, carrying out esterification on alkyl sulfonyl chloride, reacting an obtained reaction product with ethylenediamine, removing an amino protective group by hydrogen chloride to obtain the S-1-(4-ethyoxylbenzyl)-3-azapentane-1,5-diaminetrihydrochloride. The preparation method has the advantages of simplicity in operation, mild reaction condition, safety, controllability, high reaction yield and good product purity, and is more suitable for industrial production.
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Paragraph 0058; 0059
(2016/10/07)
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