ACCEPTED MANUSCRIPT
2,6-diethylaniline (10 mL, 60.7 mmol) and triethylamine (1 equiv., 8.5 mL, 60.7 mmol)
were dissolved in dry THF (80 mL). After cooling down the solution at 0 °C, 6.8 mL of
ethyl chloroacetate (1 equiv., 60.7 mmol) was added dropwise leading to a formation of
smoke and white solid. The solution was allowed to warm up at room temperature and
stirred overnight. The solid was filtered off and the organic phase was washed with
HCl 2M (2x100 mL). The aqueous phase was then washed with EtOAc and the
combined organic phases were washed with brine, dry over MgSO and dry under
4
vacuum to afford N-(2,6-diethylphenyl)-oxanilic acid ethyl ester 1b as white solid (11.23
1
g, 75% yield). H NMR (500.13 MHz, chloroform-d):
δ
8.40 (s, 1H, NH), 7.27 (t, J = 7.6 Hz,
-CH ), 2.59
), 1.20 (t, J = 7.6 Hz, 6H,
161.0 (CO, carbimide), 155.4
(CO, ester), 141.1 5 (Cq, Ar), 130.9 (Cq, Ar), 128.6 (CH, Ar), 126.5 (CH, Ar), 63.7 (CH , O-
CH -CH ), 24.8 (CH , CH -CH ), 14.3 (CH , O-CH -CH ), 14.0 (CH , CH -CH ) ppm.
Compound 1b (10.96 g, 43.57 mmol) and 2-aminophenol (1 equiv., 4.80 mg, 43.97 mmol)
were dissolved in toluene (100 mL), and 12.3 mL of NEt (1 equiv., 87.9 mmol) was
1H, ArDep-H), 7.15 (d, J = 7.6 Hz, 2H, ArDep-H), 4.44 (q, J = 7.2 Hz, 2H, O-CH
(q, J = 7.6 Hz, 4H, CH -CH ), 1.45 (t, J = 7.2 Hz, 3H, O-CH -CH
CH -CH
) ppm. 13C NMR (125.77 MHz, chloroform-d):
2
3
2
3
2
3
2
3
δ
2
2
3
2
2
3
3
2
3
3
2
3
3
added under inert atmosphere. The suspension was stirred and heated to reflux
overnight. After cooling down the solution a precipitate was obtained, which was
dissolved in dichloromethane. The solution was washed with 2 M HCl (2x100 mL). The
aqueous phase was then washed with dichloromethane and the combined organic
phases were washed with brine, dried over MgSO and dried under vacuum. The solid
4
was crystallized from warm toluene to afford N-(2,6-diethylphenyl)-N’-(2-
1
hydroxyphenyl)-oxalamide 2b (10.06 g, 73% yield). H NMR (500.13 MHz, chloroform-
d):
δ 9.68 (s, 1H, NH), 8.88 (s, 1H, NH), 8.06 (s, 1H, OH), 7.50 (dd, J = 8.1 Hz, J = 1.4 Hz,
1H, ArDep-H), 7.30 (m, 1H, Ar-H), 7.18 (s, 1H, ArDep-H), 7.17 (s, 1H, ArDep-H), 7.15 (m, 1H,
Ar-H), 6.97 (dd, J = 8.1 Hz, J = 1.4 Hz, 1H, ArDep-H), 6.92 (m, 1H, Ar-H), 2.61 (q, J = 7.6
Hz, 4H, CH
2
-CH
3
), 1.21 (t, J = 7.6 Hz, 6H, CH
2
-CH ) ppm.
3
Following the procedure described for 3aMe, the reaction of 2b (1.92 g, 6 mmol) and 49.2
1
mL of BH
3
-THF (8 equiv., 1M in THF) yielded 3b (1.6 g, 81% yield) as a white solid. H
NMR (500.13 MHz, chloroform-d):
δ
8.96 (s, 1H, NCHN), 7.57 (d, J = 8.2 Hz, 1H, ArDep-
H), 7.41 (t, J = 7.8 Hz, 1H, Ar-H), 7.20 (d, J = 7.8 Hz, 2H, ArDep-H), 7.10 (d, J = 7.8 Hz, Ar-
H), 6.96 (t, J = 7.7 Hz, 1H, Ar-H), 6.77 (t, J = 7.7 Hz, 1H, Ar-H), 4.86 (bt, J = 10.4 Hz, 2H,
NCH
Hz, 6H, CH
(Cipso, O-Ar), 141.6 (Cq, Ar), 131.8 (Cq, Ar), 131.2 (Cq, Ar), 128.8 (CH, Ar), 127.6 (CH, Ar),
122.7 (CH, Ar), 120.3 (CH, Ar), 119.9 (CH, Ar), 118.9 (CH, Ar), 51.5 (NCH ), 51.0 (NCH ),
24.3 (CH , CH -CH ), 15.2 (CH , CH -CH
) ppm. DRIFT (ν/cm-1): 2971s, 2959s, 2869s,
2
), 4.42 (bt, J = 10.4 Hz, 2H, NCH
2
), 2.64 (q, J = 7.5 Hz, 4H, CH
2
-CH
3
), 1.22 (t, J = 7.5
2
-CH
3
) ppm. 13C NMR (125.77 MHz, chloroform-d):
δ 157.2 (NCHN), 150.0
2
2
2
2
3
3
2
3
1624vs, 1588w, 1555w, 1525w, 1494w, 1476w, 1457m, 1421m, 1385w, 1368w, 1337w,
1313m, 1292s, 1284m, 1263s, 1186w, 1166w, 945w, 880w, 812m, 763w, 593w, 487w, 455w.
Anal. Calcd for C19
H
23ClN O: C, 68.97; H, 7.01; N 8.47. Found: C, 68.79; H, 7.26; N, 8.36.
2
4.3. Preparation of bis-ligated o-hydroxyaryl substituted NHC titanium(IV) complexes
15