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CasNo： 917389-32-3
Disclosed is an enantioselective process...
Disclosed herein is a novel process for ...
A palladium-catalyzed asymmetric intramo...
The development of a concise asymmetric ...
(S)-methyl 2-(8-fluoro-3-(2-methoxy-5-(trifluoromethyl)phenyl)-2-(4-(3-methoxyphenyl)piperazin-1-yl)-3,4-dihydroquinazolin-4-yl)acetate (2S,3S)-2,3-bis((4-methylbenzoyl)oxy)succinate ethyl acetate
(S)-2-(8-fluoro-3-(2-methoxy-5-(trifluoromethyl)-phenyl)-2-(4-(3-methoxyphenyl)piperazin-1-yl)-3,4-dihydroquinazolin-4-yl)acetic acid
| Conditions | Yield |
|---|---|
|
(S)-methyl 2-(8-fluoro-3-(2-methoxy-5-(trifluoromethyl)phenyl)-2-(4-(3-methoxyphenyl)piperazin-1-yl)-3,4-dihydroquinazolin-4-yl)acetate (2S,3S)-2,3-bis((4-methylbenzoyl)oxy)succinate ethyl acetate;
With
disodium hydrogenphosphate; tert-butyl methyl ether;
In
water;
for 2h;
With
sodium hydroxide;
In
water;
at 60 ℃;
for 5h;
Inert atmosphere;
|
94% |
|
(S)-methyl 2-(8-fluoro-3-(2-methoxy-5-(trifluoromethyl)phenyl)-2-(4-(3-methoxyphenyl)piperazin-1-yl)-3,4-dihydroquinazolin-4-yl)acetate (2S,3S)-2,3-bis((4-methylbenzoyl)oxy)succinate ethyl acetate;
With
sodium phosphate dibasic dihydrate; water;
In
tert-butyl methyl ether;
at 20 ℃;
for 0.666667h;
With
water; potassium hydroxide;
In
methanol; tert-butyl methyl ether;
at 50 ℃;
for 6h;
|
92% |
![(2S,3S)-2,3-bis[(4-methylbenzoyl)oxy]succinic acid {(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-(2-methoxy-5-(trifluormethyl)phenyl)-3,4-dihydroquinazolin-4-yl}acetic acid methyl ester](/upload/2025/4/f174d89b-964c-404b-bc6a-13042b79b1e3.png)
(2S,3S)-2,3-bis[(4-methylbenzoyl)oxy]succinic acid {(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-(2-methoxy-5-(trifluormethyl)phenyl)-3,4-dihydroquinazolin-4-yl}acetic acid methyl ester
(S)-2-(8-fluoro-3-(2-methoxy-5-(trifluoromethyl)-phenyl)-2-(4-(3-methoxyphenyl)piperazin-1-yl)-3,4-dihydroquinazolin-4-yl)acetic acid
| Conditions | Yield |
|---|---|
|
With
water; sodium hydrogencarbonate; sodium hydroxide;
In
tert-butyl methyl ether;
Reflux;
Large scale;
|
96.4% |
|
With
water; sodium hydrogencarbonate; sodium hydroxide;
In
tert-butyl methyl ether;
at 22 ℃;
Reflux;
Large scale;
|
96.4% |
|
With
water; sodium hydrogencarbonate;
In
tert-butyl methyl ether;
Large scale;
|
96.4% |
|
(2S,3S)-2,3-bis[(4-methylbenzoyl)oxy]succinic acid {(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-(2-methoxy-5-(trifluormethyl)phenyl)-3,4-dihydroquinazolin-4-yl}acetic acid methyl ester;
With
sodium phosphate dibasic dihydrate;
In
tert-butyl methyl ether; water;
at 20 ℃;
for 0.666667h;
With
potassium hydroxide;
In
methanol; tert-butyl methyl ether; water;
at 50 ℃;
for 6h;
With
hydrogenchloride;
In
tert-butyl methyl ether; water;
pH=4 - 5;
|
92% |
|
(2S,3S)-2,3-bis[(4-methylbenzoyl)oxy]succinic acid {(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-(2-methoxy-5-(trifluormethyl)phenyl)-3,4-dihydroquinazolin-4-yl}acetic acid methyl ester;
With
water; sodium hydrogencarbonate;
In
ethyl acetate;
With
sodium hydroxide; water;
In
1,4-dioxane;
at 20 ℃;
for 3 - 18h;
With
hydrogenchloride; water;
In
1,4-dioxane; isobutyl methyl ether;
pH=7.0 - 7.5;
Product distribution / selectivity;
|
81.2% |
(2S,3S)-2,3-bis[(4-methylbenzoyl)oxy]succinic acid {(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-(2-methoxy-5-(trifluormethyl)phenyl)-3,4-dihydroquinazolin-4-yl}acetic acid methyl ester
(R)-methyl 2-(8-fluoro-3-(2-methoxy-5-(trifluoromethyl)phenyl)-2-(4-(3-methoxyphenyl)piperazin-1-yl)-3,4-dihydroquinazolin-4-yl)acetate
methyl 2-(8-fluoro-3-(2-methoxy-5-(trifluoromethyl)phenyl)-2-oxo-1,2,3,4-tetrahydroquinazolin-4-yl)acetate
2-Fluoroaniline
