35 results about "5-azacytosine" patented technology

Oligonucleotide analogues are provided that incorporate 5-aza-cytosine in the oligonucleotide sequence, e.g., in the form of 5-aza-2′-deoxycytidine (decitabine) or 5-aza-cytidine. In particular, oligonucleotide analogues rich in decitabine-deoxyguanosine islets (DpG and GpD) are provided to target the CpG islets in the human genome, especially in the promoter regions of genes susceptible to aberrant hypermethylation. Such analogues can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position. Methods for synthesizing these oligonucleotide analogues and for modulating nucleic acid methylation are provided. Also provided are phosphoramidite building blocks for synthesizing the oligonucleotide analogues, methods for synthesizing, formulating and administering these compounds or compositions to treat conditions, such as cancer and hematological disorders.

The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: The method involves the silylation of 5-azacytosine, followed by the coupling of silylated 5-azacytosine to a protected β-D-ribofuranose derivative. The coupling reaction is catalyzed by trimethylsilyl trifluoromethanesulfonate (TMS-Triflate).

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 relates to a preparation, separation and purification method of Decitabine, which adopts the following technical scheme: taking 2'-Deoxy-D-ribose and 5-Azacytosine as basic raw materials, and preparing the Decitabine by reactions of methylation, acylation, trimethyl silylation, condensation, deprotection and the like and chiral separation and purification. The method utilizes cheap chemical products as raw materials, has mild reaction conditions, adopts a simple and easy chiral separation method, and obtains a high purity product with the chemical purity of above 99.8% and optical purity of above 99.68%, thus greatly lowering production cost and being suitable for industrialized production.

The invention discloses a 5-azacytosine synthesis method .The method comprises the following steps that 1, dicyandiamide, formic acid and a catalyst p-toluenesulfonic acid are added into an airtight reaction device and heated to react to obtain emulsion matter; 2, the product obtained in the step 1 is refined through hydrochloric acid to obtain the 5-azacytosine .A high-pressure reaction kettle is utilized, under the p-toluenesulfonic acid catalysis condition, the dehydration reaction temperature of guanylurea formate is effectively lowered, anhydrous formic acid in a system is directly utilized as a dehydrating agent, the steps of a synthesis process are simplified, side reactions are reduced, the product quality is ensured, the productivity is improved, and reaction yield is higher than 80% based on dicyandiamide .

The present invention provides 5-azacytosine derivatives with antiviral activity, specifically having viral replication inhibiting properties, more particularly in DNA viruses such as pox-, papilloma- and herpes viruses in humans. The invention also provides pharmaceutical compositions comprising such 5-azacytosine derivatives as active ingredients in combination with pharmaceutically acceptable carriers, which are useful for the treatment of subjects suffering from viral infections.

The invention provides a preparation method of a beta-configuration decitabine precursor. The preparation method comprises the following step: under the action of a Lewis acid catalyst, directly performing a coupling reaction on acylated sugar adopting the structure of 1-alkenylmethoxy-2-deoxy-3, 5-di-O-acetyl-D-ribofuranose and a silicon ether compound of 5-azacytosine to obtain beta-configuration 1-(2-deoxy-3,5-di-O-acetyl-D-ribose)-4-amino-1,3,5-s-triazine-2-one. The beta-configuration decitabine precursor is high in selectivity, good in repeatability and very high in molar yield and purity.

The invention discloses a preparation method of carbon nitride, which comprises the following step: carrying out high-temperature annealing on 5-azacytosine in a non-oxidizing atmosphere to prepare the carbon nitride, wherein the heating rate is 0.2-10 DEG C / minute, the annealing temperature is 400-700 DEG C, and the annealing time is 2-8 hours. The method can be used for preparing the high-specific-area carbon nitride material under the condition of no template, and thus, has the advantages of simplified technique, no template, one-step preparation and the like.

The invention relates to a preparation method for 5-azacytosine. The preparation method comprises: firstly reacting formic acid with a part of dicyandiamide at 50-60 DEG C, adding the residual dicyandiamide in batches after the reaction is steady, reacting at a constant temperature of 50-60 DEG C for 4 h, then heating to 100-110 DEG C and reacting for 1 h, adding acetic anhydride by dividing into two times, raising the temperature and performing refluxing reaction for 2 h, cooling to 60-70 DEG C, adding ethanol, continuing to cool to room temperature, filtering to obtain a 5-azacytosine crude product, then adding a mixed solution of ethyl acetate and ethanol, filtering and baking to dry, so as to obtain the 5-azacytosine finished product. The beneficial effects comprise that the prepared 5-azacytosine has the HPLC purity of 98.5% or more, has the impurity 1 content less than 0.5% and the impurity 2 content less than 0.1%, and the preparation method is good in technological safety, free of technological wastewater and suitable for large-scale industrialized production.