Mesylate Explained

In organosulfur chemistry, a mesylate is any salt or ester of methanesulfonic acid . In salts, the mesylate is present as the anion. When modifying the international nonproprietary name of a pharmaceutical substance containing the group or anion, the spelling used is sometimes mesilate (as in imatinib mesilate, the mesylate salt of imatinib).[1]

Mesylate esters are a group of organic compounds that share a common functional group with the general structure, abbreviated, where R is an organic substituent. Mesylate is considered a leaving group in nucleophilic substitution reactions.[2]

Preparation

Mesylate esters are generally prepared by treating an alcohol and methanesulfonyl chloride in the presence of a base, such as triethylamine.[3]

Mesyl

Related to mesylate is the mesyl (Ms) or methanesulfonyl (CH3SO2) functional group. The shortened term itself was coined by Helferich et al. in 1938 similarly to tosyl adopted earlier.[4] Methanesulfonyl chloride is often referred to as mesyl chloride.

Whereas mesylates are often hydrolytically labile, mesyl groups, when attached to nitrogen, are resistant to hydrolysis.[5] This functional group appears in a variety of medications, particularly cardiac (antiarrhythmic) drugs, as a sulfonamide moiety. Examples include sotalol, ibutilide, sematilide, dronedarone, dofetilide, E-4031, and bitopertin.

Natural occurrence

Ice core samples from a single spot in Antarctica were found to have tiny inclusions of magnesium methanesulfonate dodecahydrate. This natural phase is recognized as the mineral ernstburkeite. It is extremely rare.[6] [7]

See also

Notes and References

  1. . International Nonproprietary Names Modified . INN Working Document 05.167/3 . February 2006 . 5 December 2008.
  2. Book: Michael B. . Smith . Jerry . March . March's Advanced Organic Chemistry . John Wiley & Sons . 2007 . 6th . 978-0-471-72091-1 . 497 .
  3. (a procedure illustrating the use of mesylates).
  4. Helferich . Burckhardt . Gnüchtel . Alfred . 1938-04-06 . Ester der Methansulfonsäure in der Zuckergruppe . Berichte der deutschen chemischen Gesellschaft (A and B Series) . de . 71 . 4 . 712–718 . 10.1002/cber.19380710403 . 0365-9488.
  5. Valerie Vaillancourt, Michele M. Cudahy, Matthew M. Kreilein and Danielle L. Jacobs "Methanesulfonyl Chloride" in E-EROS Encyclopedia for Reagents in Organic Synthesis.
  6. Ernstburkeite, Mg(CH3SO3)2·12H2O, a new mineral from Antarctica . Güner, Fatma Elif Genceli . Sakurai, Toshimitsu . Hondoh, Takeo . European Journal of Mineralogy . 25 . 1 . 2013 . 78–83 . 10.1127/0935-1221/2013/0025-2257 . 2013EJMin..25...78G .
  7. http://www.mindat.org/min-41897.html Ernstburkeite