Corey–Winter olefin synthesis explained

The Corey–Winter olefin synthesis (also known as Corey–Winter–Eastwood olefination) is a series of chemical reactions for converting 1,2-diols into olefins.[1] [2] [3] [4] It is named for the American chemist and Nobelist Elias James Corey and the American-Estonian chemist Roland Arthur Edwin Winter.[5]

Often, thiocarbonyldiimidazole is used instead of thiophosgene as shown above, since thiophosgene has a similar toxicity profile as phosgene, whereas thiocarbonyldiimidazole is a much safer alternative.

Mechanism

The reaction mechanism involves the formation of a cyclic thiocarbonate from the diol and thiophosgene. The second step involves treatment with trimethyl phosphite, which attacks the sulfur atom, producing S=P(OMe)3 (driven by the formation of a strong P=S double bond) and leaving a carbene.[6] This carbene collapses with loss of carbon dioxide to give the olefin.

An alternative mechanism does not involve a free carbene intermediate, but rather involves attack of the carbanion by a second molecule of trimethylphosphite with concomitant cleavage of the sulfur-carbon bond. The phosphorus stabilized carbanion then undergoes an elimination to give the alkene, along with an acyl phosphite, which then decarboxylates.

The Corey-Winter olefination is a stereospecific reaction: a trans-diol gives a trans-alkene, while a cis-diol gives a cis-alkene as the product. For instance, cis- and trans-1,2-cyclodecanediol gives the respective cis- and trans-cyclodecene.

Notes and References

  1. Corey . E. J. . Winter . R. A. E. . Elias James Corey . A New, Stereospecific Olefin Synthesis from 1,2-Diols . . 1963 . 85 . 17 . 2677–2678 . 10.1021/ja00900a043.
  2. Corey . E. J. . Carey . F. A. . Winter . R. A. E. . Stereospecific Syntheses of Olefins from 1,2-Thionocarbonates and 1,2-Trithiocarbonates. trans-Cycloheptene . J. Am. Chem. Soc. . 1965 . 87 . 4 . 934–935 . 10.1021/ja01082a057.
  3. Corey . E. J. . Hopkins . J. . A mild procedure for the conversion of 1,2-diols to olefins . . 1982 . 23 . 19 . 1979–1982 . 10.1016/S0040-4039(00)87238-X.
  4. Crank . G. . Eastwood . F. W. . Derivatives of orthoacids. II. The preparation of olefins from 1,2-diols . Australian Journal of Chemistry . 1964 . 17 . 12 . 1392–1398 . 10.1071/CH9641392.
  5. Block, E. Org. React. 1984, 30, 457.
  6. Horton, D.; Tindall, Jr., C. G. J. Org. Chem. 1970, 35(10), 3558-3559.