cas 406482-19-7, 2-FLUORO-5-METHOXYPHENYLBORONIC ACID | Articles data ｜lookchem

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406482-19-7

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Fast and Tight Boronate Formation for Click Bioorthogonal Conjugation
A new click bioorthogonal reaction system was devised to enable the fast ligation (kON≈340 m-1 s-1) of conjugatable derivatives of a rigid cyclic diol (nopoldiol) and a carefully optimized boronic acid partner, 2-methyl-5-carboxymethylphenylboronic acid. Using NMR and fluorescence spectroscopy studies, the corresponding boronates were found to form reversibly within minutes at low micromolar concentration in water, providing submicromolar equilibrium constant (Keq≈105-106 m-1). Efficient protein conjugation under physiological conditions was demonstrated with model proteins thioredoxin and albumin, and characterized by mass spectrometry and gel electrophoresis.
Akgun, Burcin,Hall, Dennis G.
supporting information
p. 3909 - 3913
(2016/03/19)

General method for the synthesis of substituted phenanthridin-6(5H)-ones using a KOH-mediated anionic ring closure as the key step
Substituted phenanthridin-6(5H)-ones were obtained in a two-step procedure involving a Suzuki cross-coupling reaction followed by a KOH-mediated anionic ring closure. The influence of the nature and the position of the substituents on the cyclization step were studied. This methodology offers a general and practical route to diversely substituted phenanthridin-6(5H)-ones.
Dubost, Emmanuelle,Magnelli, Rosa,Cailly, Thomas,Legay, Rémi,Fabis, Frédéric,Rault, Sylvain
experimental part
p. 5008 - 5016
(2010/08/13)

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Chemical Properties

Melting Point: 194-196 °C(lit.)
Boiling Point: 333.1 °C at 760 mmHg
Flash Point:155.2 °C
Density: 1.26 g/cm³
Storage Temp.:under inert gas (nitrogen or Argon) at 2-8°C
Vapor Pressure: 5.55E-05mmHg at 25°C
Refractive Index: 1.503
PKA: 7.90±0.58(Predicted)
PSA: 49.69000
LogP: -0.48590

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