1222010-47-0Relevant articles and documents
Synthesis of Benzoxaboroles by ortho-Oxalkylation of Arylboronic Acids with Aldehydes/Ketones in the Presence of Br?nsted Acids
Zhao, Jing,Chen, Jiuxi,Xu, Qing,Li, Huan
, p. 1986 - 1990 (2021)
Herein we describe a simple and efficient synthesis of benzoxaboroles from arylboronic acids and aldehydes or ketones in the presence of a Br?nsted acid. This method greatly simplifies the starting materials and reduces the number of reaction steps. The reaction can also be accomplished with acetals and ketals. The reaction has a wide substrate scope and high practicability.
Synthesis method of benzoxaborole
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Paragraph 0044-0050, (2021/04/10)
The invention belongs to the technical field of organic synthesis, and particularly relates to a synthesis method of benzoxaborole. The synthesis method comprises the step of in an organic solvent, under the condition of a strong acid catalyst, carrying out dehydration condensation reaction on a compound shown in a formula (A) and a compound shown in a formula (B) to obtain a compound shown in a formula (C). The compounds shown in the formulas (A) and (B) and the reaction solvent in the raw materials for preparing the benzoxaborole by adopting the method are simple and easy to obtain; the reaction steps are simple, and the product can be obtained by only one step; the reaction atom economy is high, and the reaction conditions are mild; and the reaction is suitable for mass production.
1 -HYDROXY-BENZOOXABOROLES AS ANTIPARASITIC AGENTS
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Page/Page column 37, (2014/10/03)
Provided are compounds useful for controlling endoparasites both in animals and agriculture. Further provided are methods for controlling endoparasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling endoparasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. The claimed compounds are described by the following Markush formula:A typical example for a compound according to above formula is: A typical example for a compound according to above formula is:
BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS
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, (2011/05/06)
This invention provides novel compounds of the following formula useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
Design, synthesis, and structure-activity relationship of trypanosoma brucei leucyl-tRNA synthetase inhibitors as antitrypanosomal agents
Ding, Dazhong,Meng, Qingqing,Gao, Guangwei,Zhao, Yaxue,Wang, Qing,Nare, Bakela,Jacobs, Robert,Rock, Fernando,Alley, Michael R. K.,Plattner, Jacob J.,Chen, Guoqiang,Li, Dawei,Zhou, Huchen
, p. 1276 - 1287 (2011/05/07)
African trypanosomiasis, caused by the proto zoal pathogen Trypanosoma brucei (T. brucei), is one of the most neglected tropical diseases that are in great need of new drugs. We report the design and synthesis of T. brucei leucyl-tRNA synthetase (TbLeuRS) inhibitors and their structure-activity relationship. Benzoxaborole was used as the core structure and C(6) was modified to achieve improved affinity based on docking results that showed further binding space at this position. Indeed, compounds with C(7) substitutions showed diminished activity due to clash with the eukaryote specific I4ae helix while substitutions at C(6) gave enhanced affinity. TbLeuRS inhibitors with IC 50 as low as 1.6 μM were discovered, and the structure-activity relationship was discussed. The most potent enzyme inhibitors also showed excellent T. brucei parasite growth inhibition activity. This is the first time that TbLeuRS inhibitors are reported, and this study suggests that leucyl-tRNA synthetase (LeuRS) could be a potential target for antiparasitic drug development.
BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENTS
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, (2010/04/30)
This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
Discovery of novel benzoxaborole-based potent antitrypanosomal agents
Ding, Dazhong,Zhao, Yaxue,Meng, Qingqing,Xie, Dongsheng,Nare, Bakela,Chen, Daitao,Bacchi, Cyrus J.,Yarlett, Nigel,Zhang, Yong-Kang,Hernandez, Vincent,Xia, Yi,Freund, Yvonne,Abdulla, Maha,Ang, Kean-Hooi,Ratnam, Joseline,McKerrow, James H.,Jacobs, Robert T.,Zhou, Huchen,Plattner, Jacob J.
scheme or table, p. 165 - 169 (2010/10/21)
We report the discovery of benzoxaborole antitrypanosomal agents and their structure?activity relationships on central linkage groups and different substitution patterns in the sulfur-linked series. The compounds showed in vitro growth inhibition IC5
