C. Dell'Erba et al. / Tetrahedron 56 (2000) 4565±4573
4571
each, two partly overlapped d, J6.8 Hz each), 2.10 (3H, s),
3.40 (2H, hept, J6.8 Hz), 4.92 (1H, d, J1.4 Hz), 5.42
(1H, d, J1.4 Hz), 7.15 (2H, m), 7.33 (1H, m). Found: C,
78.0; H, 9.0% (C16H22O2 requires: C, 78.1; H, 8.9%).
1-(2,6-Diisopropylphenyl)-1-propenyl propionate (4c).
1H NMR (in mixed chromatographic fractions with
DP2c): d 1.15 and 1.17 [9H in all, partly overlapped t
(3H, J7.6 Hz) and d (6H, J6.8 Hz)], 1.23 (6H, d, J
6.8 Hz), 1.73 (3H, d, J6.8 Hz), 2.40 (2H, q, J7.6 Hz),
3.48 (2H, hept, J6.8 Hz), 5.23 (1H, q, J6.8 Hz), 7.14
(2H, m), 7.30 (1H, m).
Scheme 2.
2,6-Dimethylpropiophenone (DM2c). Pale-yellow oil
(50%), distilled bulb-to-bulb at 1258C/0.5 mmHg (lit.:19
General procedure for the synthesis of the alkyl
2,6-dialkylphenyl ketones DM2c±DP3c
1
bp 120±1218C/21 mmHg). H NMR: d 1.20 (3H, t, J
7.2 Hz), 2.21 (6H, s), 2.72 (2H, q, J7.2 Hz), 7.00 (2H,
m), 7.15 (1H, m). 13C NMR: d 7.55, 19.06, 37.80, 127.67,
128.38, 132.36, 142.60, 211.15. IR: 1700.0 cm21 (CvO).
Found: C, 81.3; H, 8.7% (C11H14O requires: C, 81.4; H, 8.7%).
In a ¯ame-dried 100 mL three-neck ¯ask, equipped with a
thermometer, an argon inlet, a rubber septum, and a
magnetic stirring bar, the appropriate acyl chloride
(R0COCl, 62 mmol) was dissolved in 28 mL of THF and
cooled to 08C with an external ice bath. The freshly prepared
Grignard reagent (6.2 mmol) in THF was slowly added by
cannula under magnetic stirring. The reaction mixture was
kept at 08C for 2.5 h, then poured into ice/5% HCl. After
extraction with diethyl ether the organic phase was washed
with saturated aqueous NaHCO3, then with brine to
neutrality, dried (Na2SO4) and evaporated to dryness. The
residue was chromatographed on silica gel. The desired
ketone was generally accompanied by variable amounts of
secondary products whose nature depends on the acyl
chloride. Thus, in the reactions with propionyl (R0Et)
and isobutyryl (R0Pri) chlorides the crude ketone from
chromatography was contaminated by the corresponding
2,6-dialkylphenyl ester (2,6-R2C6H3OCOR0); such
compounds could be almost completely removed by trans-
esteri®cation (EtONa/EtOH, re¯ux, 1 day) followed by
chromatography. The formation of the acetophenones
DE1c and DP1c (R0Me) as well as of the propiophenone
DP2c (R0Et) was accompanied by that of the correspond-
ing enol esters 4 (22, 30 and 29%, respectively, as deter-
mined by 1H NMR analysis of mixed chromatographic
fractions), originating from acylation of the enol of the
expected ketone with the excess acyl chloride; acid hydro-
lysis (50% H2SO4, re¯ux, 15±20 h) allowed, after usual
work up and chromatographic separation, to recover the
relevant ketone (see Scheme 2).
2,6-Dimethylisobutyrophenone (DM3c). Colourless oil
(66%), distilled bulb-to bulb at 1258C/0.5 mmHg. 1H
NMR: d 1.19 (6H, d, J6.9 Hz), 2.22 (6H, s), 2.98 (1H,
hept, J6.9 Hz) 7.02 (2H, m), 7.16 (1H, m). 13C NMR: d
17.87, 19.65, 42.16, 127.83, 128.46, 133.13, 141.80, 214.04.
IR: 1693.0 cm21 (CvO). Found: C, 81.8; H, 9.0% (C12H16O
requires: C, 81.8; H, 9.1%).
2,6-Diethylacetophenone (DE1c). Colourless oil (30%),
distilled bulb-to bulb at 1258C/0.5 mmHg (lit.:20 bp 85±
1
868C/5 mmHg). H NMR: d 1.21 (6H, t, J7.6 Hz), 2.50
and 2.53 [7H in all, s overlapped to a quartet (J7.6 Hz)],
7.08 (2H, m), 7.26 (1H, m). 13C NMR: d 15.71, 26.11,
33.01, 126.04, 128.79, 138.51, 141.72, 208.31. IR:
1695.0 cm21 (CvO). Found: C, 81.7; H, 9.2% (C12H16O
requires: C, 81.8; H, 9.1%).
2,6-Diethylpropiophenone (DE2c). Colourless oil (34%),
distilled bulb-to bulb at 1408C/0.5 mmHg. 1H NMR: d 1.20
(9H, t, J7.5 Hz), 2.47 (4H, q, J7.5 Hz), 2.72 (2H, q,
J7.5 Hz), 7.08 (2H, m), 7.26 (1H, m). 13C NMR: d 7.64,
15.73, 26.12, 38.71, 125.93, 128.72, 138.72, 141.64, 211.12.
IR: 1698.0 cm21 (CvO). Found: C, 82.0; H, 9.5% (C13H18O
requires: C, 82.1; H, 9.5%).
2,6-Diethylisobutyrophenone (DE3c). Colourless oil
(42%), distilled bulb-to-bulb at 1408C/0.5 mmHg. 1H
NMR: d 1.18 and 1.21 [12H in all, d (J7.0 Hz) partly
overlapped to a t (J7.5 Hz)], 2.47 (4H, q, J7.5 Hz),
2.92 (1H, hept, J7.0 Hz), 7.10 (2H, m), 7.27 (1H, m).
13C NMR: d 15.69, 18.03, 26.46, 42.67, 125.94, 128.76,
139.41, 140.68, 214.16. IR: 1693.0 cm21 (CvO). Found:
C, 82.3; H, 9.8% (C14H20O requires: C, 82.3; H, 9.9%).
The ketones DM2c±DP3c were all isolated as oils and
distilled bulb-to-bulb in a Kugelrohr apparatus (the quoted
temperature being that of the oven); when formation of the
enol ester 4 occurs, the yield reported (referred to the
bromoderivative) is inclusive of the product recovered by
hydrolysis of 4.
1-(2,6-Diethylphenyl)vinyl acetate (4a). 1H NMR (in
mixed chromatographic fractions with DE1c): d 1.21 (6H,
t, J7.6 Hz), 2.10 (3H, s), 2.77 (4H, q, J7.6 Hz), 4.93 (1H,
d, J1.5 Hz), 5.41 (1H, d, J1.5 Hz), 7.10 (2H, m), 7.26
(1H, m).
2,6-Diisopropylacetophenone (DP1c). Colourless oil
(24%), distilled bulb-to-bulb at 1408C/0.1 mmHg; solidi®ed
after distillation: mp 45.6±47.78C (lit.:20b mp 49.9±50.08C).
1H NMR: d 1.24 (12H, d, J6.8 Hz), 2.50 (3H, s), 2.73 (2H,
hept, J6.8 Hz), 7.16 (2H, m), 7.32 (1H, m). 13C NMR: d
24.34, 31.02, 33.87, 123.04, 128.96, 140.56, 143.20, 208.94.
IR: 1698.0 cm21 (CvO). Found: C, 82.4; H, 9.9% (C14H20O
requires: C, 82.3; H, 9.9%).
1-(2,6-Diisopropylphenyl)vinyl acetate (4b). White solid,
mp 50.5±52.58C (benzine). H NMR: d 1.19 and 1.22 (6H
1