34 results about "Cytimidine" patented technology

A process of synthesizing a 5-azacytosine nucleoside, such as azacitidine and decitabine, comprises coupling a silylated 5-azacytosine with a protected D-ribofuranose of formula in the presence of a sulfonic acid catalyst.

The invention discloses a synthetic method of emtricitabine intermediates, namely, (2R, 5S)-5-(5'-fluoro-cytimidine-1-group)-1, 3-oxathiolane-2-carboxylic acid-L-menthyl ester having the structural formula of (VI), (2R, 5S)-5-hydroxy-1, 3-oxathiolane-2-carboxylic acid-L-menthyl ester having the structural formula of (III) is taken as raw material to obtain chloro compounds having the structural formula of (IV) by chlorination reaction, then the chloro compounds (IV) are treated with condensation and hydrolyzation reactions with N, O-bis(trimethoxy)5-flurocytosin having the structural formula of (V), thus obtaining the (2R, 5S)-5-(5'-fluoro-cytimidine-1-group)-1, 3-oxathiolane-2-carboxylic acid-L-menthyl ester (VI). The invention uses bis(trichloromethyl) carbonic ester to replace the thionyl chloride in the prior art so as to be taken as a chlorination reagent, thus having the advantages of safe and reliable operation and environmental protection.

The invention relates to a preparation method of a novel nucleoside modifier 5'-DMTr-2'-ethoxyethyl (EOE)-5-Me-cytidine nucleoside. The method of the present invention uses the novel nucleoside modified substance 5'-DMTr-2'-EOE-thymidine as the starting material, and through processes such as reaction with chlorinating agent and triazole, ammonolysis treatment, etc., the yield is high. , to generate another novel nucleoside modification 5'-DMTr-2'-EOE-5-Me-cytidine nucleoside with high selectivity. The method of the invention can easily and economically synthesize the novel nucleoside modified 5'-DMTr-2'-EOE-5-Me-cytidine nucleoside in large quantities.

The invention discloses a novel synthesis process of capecitabine and discloses a preparation method of 2',3'-O-isopropylidene-5'-deoxy-5-fluoro-N4-(carbopentyloxy)cytimidine (compound V) serving as an intermediate. Meanwhile, the invention discloses a preparation method for obtaining capecitabine by removing a protective group from the compound serving as a raw material under the catalytic action of iodine. The method has the advantages of readily available raw materials, environmental friendliness, high yield and no heavy metal pollution, and is suitable for industrial production.

The invention relates to methods for preparing 5-Aza-2'-deoxycytidine and an intermediate product thereof. The method for preparing the preparing 5-Aza-2'-deoxycytidine comprises the following steps: a compound (shown in formula 2) is hydrolyzed under alkaline matter to remove acyl-oxygen protecting group, a diastereomeric compound (shown in formula 3) is obtained, and then the diastereomeric compound is separated by a general separation technology to obtain an isomer. The invention also relates to a compound (shown in formula 2) used as the intermediate product and a preparation method thereof, wherein the preparation method comprises the following steps: 5-Aza cytimidine is activated by a silanization method, and then makes displacement reaction with a compound (shown in formula 4), andfurther removes the protecting group to obtain the compound (shown in formula 2). The preparation method has simpler process, good reproduction quality and little toxicity and is suitable to the industrialized production; and meanwhile, used raw materials and reagent are easy to obtain.