Chemistry Reference
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O
O
Ph
Ph
O
O
HO
HO
O
O
O
1. MeOH.HCl
1. DMSO/(CF 3 CO) 2 O
2. L-selectride
60%
OH
HO
HO
AcHN
OMe
AcHN
2. PhCH(OMe) 2
p TsOH, DMF
69%
AcHN
OMe
HO
12
13
11
1. KOH, EtOH
2. H 2 O 2 ,Na 2 WO 4
3. LiAlH 4
4. Alkylation
1. KOH, EtOH
2. H 2 O 2 ,Na 2 WO 4
3. LiAlH 4
28%
1. KOH, EtOH
2. Alkylation
1. KOH, EtOH (88%)
2. Alkylation
NR 1 R 2
O
O
Ph
Ph
O
Ph
Ph
O
O
O
O
O
1. H 2 O 2 ,Na 2 W O 4
2. LiAlH 4
13%
OMe
HO
HO
HO
R 1 R 2 N
R 1 R 2 N
R 1 R 2 N
OMe
OMe
OMe
OH
16a,f,g,k
D-
15a,b,c,f,g,h
D-
17a
14a-k
α
-allo
D-
α
-manno
D-
α
-gluco
β
-gluco
a R 1 =R 2 =H
b R 1 =Et, R 2 =H
c R 1 =R 2 =Et
d R 1 =Pr, R 2 =H
e R 1 =R 2 =Pr
f R 1 =Bn, R 2 =H
g R 1 =R 2 =Bn
h R 1 =R 2 =-(CH 2 ) 5 -
i R 1 =R 2 = O
j R 1 =R 2 =CH 2 OH
k R 1 =Ts, R 2 =H
Scheme 13.6
Synthesis of aminoalcohols 14-17.
Table 13.1
Addition of diethylzinc to benzaldehyde catalyzed by aminoalcohols 14-17. a)
OH
O
ZnEt 2 / 14-17
H
Et
Entry
Ligand
R 1 /R 2
Yield
(%)
ee (%)
(configuration.)
Entry
Ligand
R 1 /R 2
Yield
(%)
ee (%) b)
(configuration)
1
14a
H/H
66
63 (S)
11
14k
H/Ts
55
19 (S)
2
14b
Et/H
68
20 (R)
12
15a
H/H
68
46 (S)
3
14c
Et/Et
91
53 (S)
13
15b
Et/H
81
17 (R)
4
14d
H/Pr
92
30 (R)
14
15c
Et/Et
93
26 (S)
5
14e
Pr/Pr
96
56 (S)
15
15f
H/Bn
74
14 (S)
6
14f
H/Bn
61
35 (R)
16
15g
Bn/Bn
71
32 (S)
7
14g
Bn/Bn
71
38 (S)
17
15h
(CH 2 ) 5
77
28 (S)
8
14h
(CH 2 ) 5
90
58 (S)
18
15i
69
28 (S)
9
14i
86
65 (S)
19
16a
H/H
94
32 (S)
10
14j
(CH 2 OH) 2
64
12 (R)
20
17a
H/H
88
21 (S)
a)
Conditions: 10 mol.% ligand, toluene, room temp.
b)
Enantiomeric excess in % and configuration of the major isomer.
 
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