412269-00-2Relevant academic research and scientific papers
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors
Zheng, Shilong,Guo, Shanchun,Zhong, Qiu,Zhang, Changde,Liu, Jiawang,Yang, Lin,Zhang, Qiang,Wang, Guangdi
, p. 149 - 154 (2018)
Despite promising therapeutic utilities for treatment of hematological malignancies, histone deacetylase inhibitor (HDACi) drugs have not proven as effective in the treatment of solid tumors. To expand the clinical indications of HDACi drugs, we developed novel boron-containing prodrugs of belinostat (2), one of which efficiently releases active 2 through a cascade of reactions in cell culture and demonstrates activities comparable to 2 against a panel of cancer cell lines. Importantly, prodrug 7 is more efficacious than belinostat in vivo, not only inhibiting the growth of tumor but also reducing tumor volumes in an MCF-7 xenograft tumor model owing to its superior biocompatibility, which suggests its clinical potential in the treatment of solid tumors.
Preparation method of high-purity beta-isomer
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Paragraph 0037; 0038, (2020/07/24)
The invention provides a preparation method for a belinostat cis-isomer. The method uses 3-phenylaminosulfonyl benzaldehyde as a starting material, a Wittig condensation reaction is performed, hydrolysis is performed, resolution is performed on an intermediate product of hydrolysis, separation and purification are performed, the obtained cis-intermediate of hydrolysis is subjected to a chlorination reaction, a hydroxylamine condensation reaction is performed, a crude product of the compound II is obtained, solvent beating purification is performed, and therefore the belinostat cis-isomer withthe purity of 98% or more is obtained. The method provided by the invention is simple and easy to operate, has a higher yield, and does not need preparative liquid phase separation and purification, and the obtained belinostat cis-isomer can be used as an impurity reference substance to be used for the inspection of belinostat related substances.
COMPOUNDS AND METHODS FOR TREATING CANCER
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, (2020/12/19)
Substituted cinnamamide compounds and analogs, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or ameliorate cancer are provided.
NOVEL PROCESS FOR THE PREPARATION OF BELINOSTAT
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Page/Page column 23; 24, (2017/12/16)
The present invention provides a novel and commercially viable process with high yield for the preparation of (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide, also known as Belinostat (I). The invention also provides process for purification and nov
A he belli department is suitable for industrial production of synthetic method
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, (2016/10/08)
The invention provides an improved belinostatsynthesis method. According to the method, sodium m-carboxyl benzenesulfonate is taken as a starting material, and belinostat is prepared through six steps of esterification, acylation and aniline condensation, reduction, oxidation, Wittig-Horner condensation and hydrolysis as well as acylation and hydroxylamine condensation. With the adoption of the method, the production time is shortened, the reaction yield is increased, the production safety is enhanced, the environmental pollution is reduced, and the method is more suitable for industrial production.
A method for preparing belli department he isomer (by machine translation)
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Paragraph 0035; 0036, (2016/10/07)
The present invention provides a kind of he belli department method for preparing cis-isomer, the method uses 3-phenyl amino sulfonyl benzald as the starting material, by Wittig condensation reaction, hydrolysis, chlorinated reaction, condensation reaction and Belinostat azanol Belinostat isomer mixture, mixture in the content of the cis-isomer Belinostat than the prior art is greatly improved. The reaction to obtain the isomer mixture Belinostat Belinostat and efficient process for preparing liquid-phase chromatography of the opposite phase separation and purification, gradient elution get purity 99% of the material above Belinostat check the requirements of the impurity in a vertebrate Belinostat isomer. (by machine translation)
Synthesis method of belinostat
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, (2016/11/14)
The invention discloses a synthesis method of belinostat. The method comprises the following steps: by using benzoic acid as an initial material, performing six reaction steps of chlorosulfonation, aniline condensation, reduction, oxidation, Witting-Horner condensation and hydrolysis, acylating chlorination and hydroxylamine condensation to prepare a target compound. The initial material benzoic acid of the method is cheap and easy to obtain, the sulfonylation and acylating chlorination reaction are realized through one step, the preparation time is shortened, and the yield is improved. In the oxidation process, an oxidizing reagent which is cheap and does not contains metal ion is adopted so that the active ingredients easily achieve the requirement of heavy metal ion limitation, and the pollution to the environment is reduced. All reaction intermediates of the method are solid and can be purified through a salt formation or recrystallization method, the time-consuming and labor-consuming column chromatography purification is avoided, and the method is suitable for industrial production.
The Development of an Effective Synthetic Route of Belinostat
Bao, Xuefei,Song, Dake,Qiao, Xuejun,Zhao, Xuan,Chen, Guoliang
, p. 1482 - 1488 (2016/08/30)
A practical synthetic route of belinostat is reported. Belinostat was obtained via a five-step process starting from benzaldehyde and including addition reaction with sodium bisulfite, sulfochlorination with chlorosulfonic acid, sulfonamidation with aniline, Knoevenagel condensation, and the final amidation with hydroxylamine. Key to the strategy is the preparation of 3-formylbenzenesulfonyl chloride using an economical and practical protocol. The main advantages of the route include inexpensive starting materials and acceptable overall yield. The scale-up experiment was carried out to provide 169 g of belinostat with 99.6% purity in 33% total yield.
METHODS OF SYNTHESIS OF CERTAIN HYDROXAMIC ACID COMPOUNDS
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Page/Page column 53-54, (2009/05/29)
The present invention pertains to the general field of chemical synthesis, and more particularly to methods for the synthesis of certain hydroxamic acid compounds, and in particular, (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide, also known as PXD
