entrya
|
catalyst |
solvent |
hydrogen donor |
yield (%) |
ee (%) |
1 |
Cat1 |
DCM |
HCO2H/Et3N
(5:2) |
<5 |
— |
2 |
Cat2 |
DCM |
HCO2H/Et3N
(5:2) |
<5 |
— |
3 |
Cat3 |
DCM |
HCO2H/Et3N
(5:2) |
99 |
98 |
4 |
Cat4 |
DCM |
HCO2H/Et3N
(5:2) |
40 |
98 |
5 |
Cat5 |
DCM |
HCO2H/Et3N
(5:2) |
<5 |
— |
6 |
Cat6 |
DCM |
HCO2H/Et3N
(5:2) |
99 |
>99 |
7b
|
Cat6 |
THF |
HCO2H/Et3N (5:2) |
57 |
>99 |
8b
|
Cat6 |
DCM |
HCO2H/Et3N (5:2) |
35 |
99 |
9b
|
Cat6 |
toluene |
HCO2H/Et3N (5:2) |
56 |
99 |
10b
|
Cat6 |
MeCN |
HCO2H/Et3N (5:2) |
54 |
99 |
11b
|
Cat6 |
MeOH |
HCO2H/Et3N (5:2) |
12 |
99 |
11b
|
Cat6 |
iPrOH |
HCO2H/Et3N (5:2) |
25 |
>99 |
12b
|
Cat6 |
THF |
HCO2H/Et3N (3:2) |
85 |
>99 |
13b
|
Cat6 |
THF |
HCO2H/Et3N (1:1) |
96 |
>99 |
14b
|
Cat6 |
THF |
HCO2H/DBU (1:1) |
99 |
>99 |
15b
|
Cat6 |
THF |
HCO2H/DIPEA (1:1) |
94 |
>99 |
16b
|
Cat6 |
THF |
HCO2Na |
17 |
>99 |
17b
|
Cat6 |
THF |
IPA |
<5 |
— |
18c
|
Cat6 |
THF |
HCO2H/DBU (1:1) |
98 |
>99 |
19d
|
Cat6 |
THF |
HCO2H/DBU (1:1) |
65 |
>99 |