A Stable Enol In Small Ring Systems: Clear Differentiation
Between Penta- and Tri-valency Of Phosphorus Atoms.
Alex S. Ionkin*, William J. Marshall, Brian M. Fish, Matthew F. Schiffhauer, Charles N.
McEwen.
Supporting Information
Syntheses of compounds: 2,3-Di-tert-butyl-1-trimethylsilanyl-4-trimethylsilanyloxy-1,2-dihydro-phosphete (3).
Lithium bis(trimethyl-silyl)phosphide as a bis(tetrahydrafuran) complex (1) (7.55 g (0.0226 mol) and 4.59 g (0.0226 mol) of trans-2-
tert-butyl-4,4-dimethyl-pent-2-enoyl chloride (2)
1
were mixed in 40 ml of pentane at the room temperature. After 3 days, the mixture
was filtered and purified by the kugelrohr distillation collecting the fraction between 32 and 38ºC at 0.1 mm of Hg. Yield of 2,3-di-
tert-butyl-1-trimethylsilanyl-4-trimethylsilanyloxy-1,2-dihydro-phosphete (3) was 4.53 g (58%) as a viscous oil.
1
H NMR (500 MHz,
CD
2
Cl
2
, TMS): δ 0.10 (s, 9H, Me-Si), 0.20 (s, 9H, Me-Si), 1.00 (s, 9H, Me), 1.10 (s, 9H, Me), 2.20 (s, 1H, CH-P).
13
C NMR (500
MHz, CD2Cl2, TMS): δ - 1.76 (s, Me-Si), 0.00 (s, Me-Si), 29.92 (s, Me), 30.02 (s, Me), 32.88 (s, C-Me), 35.00 (s, C-Me), 43.52 (d,
2
J
PC
= 10.1 Hz, HC-P), 134.34 (d,
2
J
PC
= 13.9 Hz, C=C), 144.54 (d,
2
J
PC
= 5.1 Hz, C=C).
31
P NMR (500 MHz, CD
2
Cl
2
): δ - 40.16 (s,
1P). 2,3-Di-tert-butyl-1-trimethylsilanyl-4-trimethylsilanyloxy-1,2-dihydro-phosphete (3) was identified by the mass-spectrometry
(ASAP method), which gave MH
+
ion at 345.21 corresponding to C
17
H
38
OPSi
2
.
3,4-Di-tert-butyl-1-oxo-1,4-dihydro-1λ
5
-phosphet-2-ol (6). 0.3 g of (0.00087 mol) of 2,3-di-tert-butyl-1-trimethylsilanyl-4-
trimethylsilanyloxy-1,2-dihydro-phosphete (3) was dissolved in 5 ml of methylene chloride and left on air for 3 weeks. The resultant
crystals of 3,4-di-tert-butyl-1-oxo-1,4-dihydro-1λ
5
-phosphet-2-ol (6) were formed quantitatively with m.p. 100 ºC.
1
H NMR (500
MHz, CD2Cl2, TMS): δ 1.15 (s, 9H, Me), 1.19 (s, 9H, Me), 2.95 (dd,
2
JPH = 14.7 Hz,
3
JHH = 0.8 Hz, 1H, CH-P), 7.15 (dd,
1
JPH = 495.6
Hz,
3
J
HH
= 0.8 Hz, 1H, PH), O-H proton was not observed.
13
C NMR (500 MHz, CD
2
Cl
2
, TMS): δ 29.00 (d,
4
J
PC
= 1.9 Hz, Me), 30.00
(d,
3
JPC = 8.5 Hz, Me), 33.90 (d,
2
JPC = 20.3 Hz, C-Me), 34.20 (d,
3
JPC = 16.8 Hz, C-Me), 57.20 (d,
1
JPC = 56.1 Hz, C-P), 134.30 (d,
2
JPC = 14.1 Hz, C=C), 154.60 (d,
1
JPC = 80.9 Hz, C=C).
31
P NMR (500 MHz, CD2Cl2): δ 4.17 (d,
1
JPH = 495.6 Hz, 1P). The structure
was proven by X-ray analysis.
Pyrolysis of 2,3-di-tert-butyl-1-trimethylsilanyl-4-trimethylsilanyloxy-1,2-dihydro-phosphete (3): Tris(trimethylsilyl)phosphine (8),
1,2,5,6-Tetra-tert-butyl-3,7-bis-trimethylsilanyloxy-1H,5H-[1,2]diphospholo[1,2-a][1,2]diphosphole (7) and 3,4-Di-tert-butyl-1-(2-
tert-butyl-4,4-dimethyl-pent-2-enoyl)-phosphetan-2-one (9). A 2.0 g (0.0058 mol) sample of 2,3-di-tert-butyl-1-trimethylsilanyl-4-
trimethylsilanyloxy-1,2-dihydro-phosphete (3) was placed in the kugelrohr distillation apparatus. The two receiving bulbs were cooled
by dry ice/acetone bath. Oven flask was heated to 180 °C at 1 mm of Hg and following fractions were collected.
Tris(trimethylsilyl)phosphine (8) was collected first at temperature interval 180 °C to 220 °C in oven. Yield of 8 was 0.34 g (23%) as
colorless liquid, which solidified upon standing.
31
P NMR (500 MHz, CD2Cl2): δ - 250.00 (s, 1P). The second fraction of the pyrolysis
(at temperature interval 220 °C to 260 °C in oven) crystallized upon standing yielding 1,2,5,6-tetra-tert-butyl-3,7-bis-
trimethylsilanyloxy-1H,5H-[1,2]diphospholo[1,2-a][1,2]diphosphole (7). The yield of 7 was 0.49 g (31%) with m.p. 169-172ºC.
1
H
NMR (500 MHz, CD2Cl2, TMS): δ 0.30 (s, 18H, Me-Si), 1.10 (s, 9H, Me), 1.20 (s, 9H, Me), 2.60 (br, 2H, CH-P).
13
C NMR (500
MHz, CD
2
Cl
2
): δ 1.54 (s, Me-Si), 31.10 (s, Me), 32.00 (t,
4
J
PC
+
5
J
PC
= 8.3 Hz, Me), 34.40 (s, C-Me), 38.06 (t,
1
J
PC
+
2
J
PC
= 8.9 Hz, C-
Me), 53.25 (t,
1
JPC+
2
JPC = 15.3 Hz, C-P), 137.69 (t,
2
JPC+
3
JPC = 3.4 Hz, C=C), 158.70 (t,
1
JPC+
2
JPC = 16.5 Hz, C=C).
31
P NMR (500
MHz, CD2Cl2): δ 10.60 (s, 1P). The structure was proven by X-ray analysis. 3,4-Di-tert-butyl-1-(2-tert-butyl-4,4-dimethyl-pent-2-
enoyl)-phosphetan-2-one (9) was isolated after the chromatography of the residue from the above pyrolysis. The chromatography was
done on silica gel with eluent with eluent 20% of ethyl ether and 80% of hexane. Compound 9 was additionally purified by the
sublimation of the combined chromatographic fractions at 50 ºC and 5 mm for 1 week. The yield of 3,4-di-tert-butyl-1-(2-tert-butyl-
4,4-dimethyl-pent-2-enoyl)-phosphetan-2-one (9) was 0.49 g (60%). The sample starts to sublime at 41-43ºC and completely melts at
104-106ºC.
1
H NMR (500 MHz, CD2Cl2, TMS): δ 0.98 (s, 9H, Me), 1.05 (s, 9H, Me), 1.10 (s, 9H, Me), 1.13 (s, 9H, Me), 2.85 (dd,
2
J
PH
= 6.8 Hz,
3
J
HH
= 7.0 Hz, 1H, CH-P), 3.44 (dd,
3
J
PH
= 2.4 Hz,
3
J
HH
= 7.0 Hz, 1H, CH), 5.50 (d,
4
J
PH
= 1.2 Hz, 1H, C=C-H).
13
C
NMR (500 MHz, CD
2
Cl
2
): δ 29.00 (s, Me), 29.90 (d,
3
J
PC
= 8.9 Hz, Me), 31.20 (d,
4
J
PC
= 1.7 Hz, Me), 31.40 (d,
4
J
PC
= 4.8 Hz, Me),
32.30 (d,
1
JPC = 17.4 Hz, C-H), 33.90 (s, C-Me), 35.05 (d,
2
JPC = 6.9 Hz, C-Me), 36.30 (d,
3
JPC = 1.5 Hz, C-Me), 38.90 (d,
3
JPC = 5.0
Hz, C-Me), 77.90 (d,
2
J
PC
= 21.2 Hz, C-H), 139.10 (d,
3
J
PC
= 1.7 Hz, C=C), 149.50 (d,
2
J
PC
= 32.5 Hz, C=C), 211.10 (d,
1
J
PC
= 29.5 Hz,
C=O), 211.50 (d,
1
J
PC
= 76.3 Hz, C=O).
31
P NMR (500 MHz, CD
2
Cl
2
): δ 104.00 (s, 1P). The structure was proven by X-ray analysis.
2-tert-Butyl-1-(2,3-di-tert-butyl-4-hydroxy-1-oxo-1,2-dihydro-1λ
5
-phosphet-1-yl)-4,4-dimethyl-pent-2-en-1-one (10). 1.63 g (0.0045
mol) sample of 3,4-di-tert-butyl-1-(2-tert-butyl-4,4-dimethyl-pent-2-enoyl)-phosphetan-2-one (9) and 0.85 g (0.0089 mol) of pyridine-
N-oxide were stirred in 20 ml of toluene at 90 ºC for 2 weeks. Then solvent was removed in vacuo at 1 mmHg, and the residue was
purified by the chromatography on silica gel with the eluent petroleum ether/ethyl ether, 10:2. Yield of 2-tert-butyl-1-(2,3-di-tert-
butyl-4-hydroxy-1-oxo-1,2-dihydro-1λ
5
-phosphet-1-yl)-4,4-dimethyl-pent-2-en-1-one (10) was 0.27 g (16%) as colorless crystals with
m.p. 70 ºC (decomposition).
1
H NMR (500 MHz, CD2Cl2, TMS): δ 1.05 (s, 9H, Me), 1.10 (s, 9H, Me), 1.15 (s, 9H, Me), 1.25 (s, 9H,
Me), 3.10 (br, 1H, CH-P), 5.56 (s, 1H, C=C-H), O-H proton was not observed.
13
C NMR (500 MHz, CD2Cl2, selected signals): δ
218.00 (d,
1
J
PC
= 53.9 Hz, P-C=O).
31
P NMR (500 MHz, CD
2
Cl
2
): δ 17.9 (s, 1P). The structure was proven by X-ray analysis.
1 A. S. Ionkin, W. J. Marshall, B. M. Fish, Org. Lett. 2008, 10, 2303.
Supplementary Material (ESI) for Chemical Communications
This journal is © The Royal Society of Chemistry 2008