Radical-mediated desulfonylation reactions with group 14 metallo hydrides : synthesis of (a-fluoro)phosphonates and (a-fluoro)vinyl silanes

Document Type

Thesis

Degree

Master of Science (MS)

Major/Program

Chemistry

First Advisor's Name

Stanislaw F. Wnuk

First Advisor's Committee Title

Committee Chair

Second Advisor's Name

Kathleen Rein

Third Advisor's Name

Fenfei Leng

Date of Defense

7-21-2004

Abstract

The sulfone group is a well-established activating moiety important in many organic transformations. Standard procedures for desulfonylation [Al(Hg), or Na(Hg)] were ineffective for the removal of the pyridin-2-ylsulfonyl group from the α-carbon of phosphonic esters. Prompted by these results, we undertook a study for the synthesis of α-(arylsulfonyl)phosphonates, and their fluorination with Selectfluor to produce α-fluoro-α-(arylsulfonyl)phosphonates, Radical mediated hydrogenolysis of α-fluoro-α-(arylsulfonyl)phosphonates using BujSnH gave (α-fluoro)phosphonates. We observed that the yield for the desulfonylation reaction depends on the n-deficiency effect and increase in the order pyrimidinyl > pyridinyl > phenyl sulfonyl.

The (α-fluoro)phosphonates were employed as convenient precursors in the Homer-Wadsworth-Emmons (HWE) reaction to provide (α-fluoro)vinyl sulfones. The vinyl and (α-fluoro)vinyl sulfones underwent substitutive silyl and germyl- desulfonylation to yield vinyl and (α-fluoro)vinyl silanes and germanes via an addition-elimination mechanism. The vinyl tris(trimethylsilyl)silanes were employed as nucleophiles (under oxidative conditions) in palladium-catalyzed cross coupling reactions with iodobenzene and bromobenzene.

Identifier

FI15101514

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