141607-09-2Relevant academic research and scientific papers
Synthesis of Highly Substituted Phenols and Benzenes with Complete Regiochemical Control
Zhang, Xiaojie,Beaudry, Christopher M.
supporting information, p. 6086 - 6090 (2020/08/12)
Substituted phenols are requisite molecules for human health, agriculture, and diverse synthetic materials. We report a chemical synthesis of phenols, including penta-substituted phenols, that accommodates programmable substitution at any position. This method uses a one-step conversion of readily available hydroxypyrone and nitroalkene starting materials to give phenols with complete regiochemical control and in high chemical yield. Additionally, the phenols can be converted into highly and even fully substituted benzenes.
Identification of a 4-fluorobenzyl L-valinate amide benzoxaborole (AN11736) as a potential development candidate for the treatment of Animal African Trypanosomiasis (AAT)
Akama, Tsutomu,Zhang, Yong-Kang,Freund, Yvonne R.,Berry, Pamela,Lee, Joanne,Easom, Eric E.,Jacobs, Robert T.,Plattner, Jacob J.,Witty, Michael J.,Peter, Rosemary,Rowan, Tim G.,Gillingwater, Kirsten,Brun, Reto,Nare, Bakela,Mercer, Luke,Xu, Musheng,Wang, Jiangong,Liang, Hao
, p. 6 - 10 (2017/11/27)
Novel L-valinate amide benzoxaboroles and analogues were designed and synthesized for a structure-activity-relationship (SAR) investigation to optimize the growth inhibitory activity against Trypanosoma congolense (T. congolense) and Trypanosoma vivax (T. vivax) parasites. The study identified 4-fluorobenzyl (1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborole-6-carbonyl)-L-valinate (5, AN11736), which showed IC50 values of 0.15 nM against T. congolense and 1.3 nM against T. vivax, and demonstrated 100% efficacy with a single dose of 10 mg/kg against both T. congolense and T. vivax in mouse models of infection (IP dosing) and in the target animal, cattle, dosed intramuscularly. AN11736 has been advanced to early development studies.
OXABOROLE ESTERS AND USES THEREOF
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Page/Page column 33, (2017/12/05)
The present invention provides oxaborole ester compounds and compositions thereof which are useful to treat diseases associated with parasites, such as Chagas Disease and African Animal Trypanosomosis.
TETRAZOLE COMPOUNDS FOR REDUCING URIC ACID
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Paragraph 0133, (2015/11/30)
Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including g
ARYL AND HETEROARYL FUSED LACTAMS
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Paragraph 0934; 0935, (2014/07/08)
This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
Judicious application of allyl protecting groups for the synthesis of 2-Morpholin-4-yl-4-oxo-4H-chromen-8-yl triflate, a key precursor of DNA-dependent protein kinase inhibitors
Aristegui, Sonsoles Rodriguez,El-Murr, Marine Desage,Golding, Bernard T.,Griffin, Roger J.,Hardcastle, Ian R.
, p. 5927 - 5929 (2007/10/03)
(Chemical Equation Presented) 2-Morpholin-4-yl-4-oxo-4H-chromen-8-yl 2,2,2-trifluoromethanesulfonate is a key intermediate for the synthesis of the DNA-dependent protein kinase (DNA-PK) inhibitor 8-dibenzothiophen-4-yl-2- morpholin-4-yl-chromen-4-one (NU7441). Two improved methods for the synthesis of this triflate have been developed: (A) in 35% overall yield, through modification of the published route, and (B) in 15% overall yield, by a new route employing a Baker-Venkataraman rearrangement to enable generation of the chromenone scaffold. Both syntheses depend on the judicious use of allyl protecting groups.
RECEPTOR FUNCTION REGULATING AGENT
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Page/Page column 112-113, (2010/11/23)
An agent for regulating 14273 receptor function, which is useful as a preventing or treating drug for diabetes mellitus, hyperlipidemia or the like, is provided. An agent for regulating 14273 receptor function comprising a compound containing an aromatic ring and a group capable of releasing a cation.
Trisubstituted benzoic acid intermediates
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, (2008/06/13)
2-methyl-3-(substituted)-4-(substituted) benzoic acids or their alkyl ester that are useful to prepare herbicidal compounds.
