- Susceptibility to hydrolysis of phenylboronic pinacol esters at physiological pH
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Boronic acids and their esters are highly considered compounds for the design of new drugs and drug delivery devices, particularly as boron-carriers suitable for neutron capture therapy. However, these compounds are only marginally stable in water. Hydrol
- Achilli, Cesare,Ciana, Annarita,Fagnoni, Maurizio,Balduini, Cesare,Minetti, Giampaolo
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Read Online
- SO2F2-Activated Efficient Beckmann Rearrangement of Ketoximes for Accessing Amides and Lactams
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A novel, mild and practical protocol for the efficient activation of the Beckmann rearrangement utilizing the readily available and economical sulfuryl fluoride (SO2F2 gas) has been developed. The substrate scope of the operationally simple methodology has been demonstrated by 37 examples with good to nearly quantitative isolated yields (over 90 % yield in most cases) in a short time, including B(OH)2, COOH, NH2, and OH substituted substrates. A tentative mechanism was proposed involving formation and elimination of key intermediate, sulfonyl ester.
- Zhang, Guofu,Zhao, Yiyong,Xuan, Lidi,Ding, Chengrong
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supporting information
p. 4911 - 4915
(2019/07/31)
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- A method of preparing 4-aminophenylboronic acid derivatives
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The invention belongs to the technical field of medicine intermediates, and particularly relates to a method of preparing 4-aminophenylboronic acid derivatives. According to the method, 4-nitrophenylboronic acid is adopted as a raw material and subjected
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Paragraph 0017; 0018; 0020
(2017/09/01)
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- Sequential one-pot access to molecular diversity through aniline aqueous borylation
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On the basis of our recently reported aniline aqueous borylation, molecular diversity was achieved in a one-pot process by combining other reactions such as esterification, Suzuki-Miyaura coupling, hydrogenolysis, or Petasis borono-Mannich.
- Erb, William,Albini, Mathieu,Rouden, Jacques,Blanchet, Jrme
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p. 10568 - 10580
(2015/01/08)
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- Synthesis and biological activity of new 4-(Pyridin-4-yl)-(3-methoxy-5- methylphenyl)- 1H-pyrazoles derivatives as ROS Receptor tyrosine kinase inhibitors
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A series of new 4-(pyridin-4-yl)-(3-methoxy-5-methylphenyl)-1H-pyrazoles (6a-k & 7a-l) has been rationally designed based on the structure of the lead compound KIST301080, a selective ROS receptor tyrosine kinase inhibitor, in order to study the activity of ROS of this new class of inhibitors. The compounds were synthesized and screened against ROS kinase, where compound 6h showed moderate inhibitory activity with an IC50 value of 6.25 μM. The study emphasized the importance of the acetonitrile group at the pyrazole ring and also the importance of having a hydrogen bond donor on the distal phenyl ring linked to the pyridine moiety.
- Park, Byung Sun,El-deeb, Ibrahim M.,Yoo, Kyung Ho,Han, Dong Keun,Tae, Jin Sung,Lee, So Ha
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p. 3629 - 3634
(2013/01/16)
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- Heterocyclic compounds
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The invention concerns pharmaceutically useful compounds of the formula I, in which A1, A2, A3, A4, B1, m, Ar, W, X, Y, Z and R1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
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