Newsletter 9 PDF Print E-mail
Newsletter N° 9 - 2nd quarter 2009

Contents :  New moleculesFocus on indazoles  |  Zoom on trifluoroborates  |  Special offer on indazoles and trifluoroborates

NEW MOLECULES
This month our product catalogue of organoboron building blocks and fine chemicals has been updated with the following new and original boronic acids and boronic esters, organotrifluoroborates, polyaromatics and halogenated heterocycles.

>> Overview of new molecules
>> Download BoroChem’s complete 2009 catalogue in PDF format

FOCUS ON INDAZOLES
Indazoles are 2-aza bioisosteres of tryptamine, serotonin, melatonin, or tryptophan. Indazoles represent a widely used medicinal chemistry pharmacophore that is found in a number of marketed drugs, including the anticancer agents BMS-599626 and GDC-0941 :

indazoles

Given the potential of indazoles to serve as valuable buidling blocks in medicinal chemistry, BoroChem has focused its R&D efforts on the synthesis of new intermediates containing the indazole moiety; boronic indazoles. In particular, several boronic acid-substituted indazoles have been targeted. The following indazolylboronic acids and boronate esters have been developed inhouse and are currently available :

        B11-0004 | 1-(Tetrahydro-2H-pyran-2-yl)-1H-indazole-5-boronic acid pinacol ester         B11-0002 | 1H-Indazole-5-boronic acid

The following is an example of a general substructure that can be customized by our laboratory. Feel free to contact us for your specific requirements.

custom synthesis of indazoles

ZOOM ON TRIFLUOROBORATES AS AN ALTERNATIVE TO MODERATELY STABLE BORONIC ACIDS
R&D chemists at BoroChem have been developing new Potassium Heteroaryltrifluoroborates, which offer great stability and excellent cross-coupling efficiency. The organotrifluoroborates are especially useful for those cases wherein the boronic acids counterparts lack stability owing to facile protodeboronation, compromising both the integrity of the reagents and the yield of the Suzuki-Miyaura cross-coupling reaction.

Further supporting information is available in the latest contribution from Professor Gary Molander’s laboratory, which was chosen as a Featured Article by the Editors of The Journal of Organic Chemistry ("Scope of the Suzuki-Miyaura Cross-Coupling reactions of Potassium Heteroaryltrifluoroborates", Gary A. Molander, Belgin Canturk, Lauren E. Kennedy, J. Org. Chem., 2009, 74 (3), pp 973–980).

For your convenience BoroChem offers several alternatives :
  • Boronic Acids (mild reaction conditions)
  • Boronic Esters (ease of purification)
  • Trifluoroborates (great air and moisture stability)
   B01-0001 | Pyridine-3-boronic acid   B01-0014 | Pyridine-3-boronic acid pinacol ester   BF2-0005 | Potassium pyridine-3-trifluoroborate   B01-0105 | Sodium pyridine-3-trihydroxyborate
             B09-0008 | 1H-Pyrazole-5-boronic acid       B09-0009 | 1H-Pyrazole-5-boronic acid pinacol ester         BF2-0008 | Potassium pyrazole-5-trifluoroborate

Taking into account the advantages of the potassium heteroaryltrifluoroborates, BoroChem will continue to expand its offering of these compounds. We also invite you to This e-mail address is being protected from spambots. You need JavaScript enabled to view it if you were interested in some specific compounds.

The above-presented organotrifluoroborates are currently available at a discount rate as part of our special offer. For more information, please see below.

SPECIAL OFFER ON INDAZOLES AND TRIFLUOROBORATES
Try any of the above-presented indazoles or compare the reactivity of a trifluoroborate against its boronic acid or ester counterpart. Choose any of the above-presented compounds at a set price of

€ 300 / 410 USD per INDAZOLE (1 g)
€ 70 / 95 USD per PYRIDINE (1 g)
€ 110 / 150 USD per PYRAZOLE (1 g)

Please mention discount code 09NL9 with your order.
This offer is valid until 26th June 2009.