|
|
wt/vol
|
MW
|
Moles
|
density
|
equivs.
|
yield
|
|
I
|
0.096 g
|
218.37
|
0.0004
|
|
1.0
|
|
|
II
|
0.077 mL
|
126.93
|
0.0009
|
1.455
|
2.0
|
|
|
III
|
0.125 mL
|
78.13
|
0.0018
|
1.101
|
4.0
|
|
|
IV
|
0.250 mL
|
101.19
|
0.0018
|
0.726
|
4.0
|
|
|
V
|
5 mL
|
-
|
-
|
|
|
|
|
VI
|
0.083 g
|
216.35
|
0.0004
|
|
|
(87%)
|
Procedure: 25 mL 1-neck flask, stirbar, septum, N2
inlet
Dissolved
0.077 mL of oxalylchloride (II) in 4.0
mL of dry CH2Cl2.
Stirred; cooled to -78 C.
Added 0.125 mL of DMSO.
Stirred 10 min. Added a
solution of 0.096 g of alcohol I
in 1.0 mL of CH2Cl2. Stirred 15 min.
Added 0.250 mL Et3N.
After 15 min, warmed to 0 C.
After 10 min TLC showed complete reaction. The reaction mixture was placed on a silica gel column and
the product was isolated by flash chromatography using 25:75 EtOAc-hexanes as
eluant. The product was a clear,
colorless oil.
1H NMR (CDCl3,
300 MHz) d 9.06 (d, J = 6.2 Hz, CHO), 3.97 (dd, J = 12.3, 2.3 Hz, H4), 3.77 (dd, J = 12.3, 3.7 Hz, H4), 3.36 (m, H2, H3), 0.87 (s,
SiC(CH3)3), 0.06 (s, SiCH3), 0.05 (s, SiCH3).
notes
The use of DMSO "activated" by oxalyl chloride has
widely become known as the Swern oxidation (see Mancuso, A.J.; Huang, S-L.;
Swern, D. J. Org. Chem. 1978,
43, 2480). A brief period of premixing of oxalyl chloride and DMSO
forms the "activated" salt to which is added the primary or secondary
alcohol.
The mechanism for the Swern oxidation as first proposed by
Corey (see Corey, E.J.; Kim, C.U. Tetrahedron
Lett.
1974, 287) is as follows.