Current location:Home > Pharmaceutical
Product
99% Purity Commercial production Darapladib 356057-34-6 with Cheapest Price
- Molecular Formula: C36H38F4N4O2S
- Molecular Weight: 666.771133
- Boiling Point: 741.002 °C at 760 mmHg
- PKA: 9.03±0.10(Predicted)
- Flash Point: 401.944 °C
- PSA: 83.74000
- Density: 1.259 g/cm3
- LogP: 7.21980
356057-34-6 Relevant articles
RADIOLABELED DARAPLADIB AND ANALOGS THEREOF AND THEIR USE AS IMAGING COMPOUNDS
-
Page/Page column 35, (2019/04/26)
The present inventors have developed new...
Regioselectivity of thiouracil alkylation: Application to optimization of Darapladib synthesis
Guibbal, Florian,Bénard, Sébastien,Patché, Jessica,Meneyrol, Vincent,Couprie, Jo?l,Yong-Sang, Jennyfer,Meilhac, Olivier,Jestin, Emmanuelle
supporting information, p. 787 - 792 (2018/01/17)
Darapladib is one of the most potent Lp-...
Compounds
-
Page/Page column 41; 42, (2016/05/11)
Pyrimidone compounds of formula (I): are...
PROCESSES FOR THE PREPARATION OF DARAPLADIB AND ITS INTERMEDIATES
-
Page/Page column 19; 20, (2015/06/25)
The present invention provides a process...
356057-34-6 Process route
-
-
304694-40-4
N,N-diethyl-N'-(4'-trifluoromethylbiphenyl-4-ylmethyl)ethane-1,2-diamine
-
-
356058-42-9
{2-[(4-fluorobenzyl)sulfanyl]-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl}acetic acid
-
-
356057-34-6
N-[2-(diethylamino)ethyl]-2-(2-{[(4-fluorophenyl)methyl]thio}-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl)-N-{[4’-(trifluoromethyl)-4-biphenylyl]methyl}acetamide
| Conditions | Yield |
|---|---|
|
With
boric acid;
In
toluene;
at 110 ℃;
for 6h;
Reagent/catalyst;
Temperature;
Solvent;
|
82.63%
|
|
With
1-hydroxy-7-aza-benzotriazole; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride;
In
N,N-dimethyl-formamide;
at 50 ℃;
for 3h;
|
78%
|
|
N,N-diethyl-N'-(4'-trifluoromethylbiphenyl-4-ylmethyl)ethane-1,2-diamine; {2-[(4-fluorobenzyl)sulfanyl]-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl}acetic acid;
With
N-ethyl-N,N-diisopropylamine;
In
N,N-dimethyl-formamide;
at 20 ℃;
for 0.166667h;
With
1-[(1-(cyano-?2-?ethoxy-?2-?oxoethylidenaminooxy)?dimethylamino-?morpholino)]-uronium hexafluorophosphate;
In
N,N-dimethyl-formamide;
at 0 - 20 ℃;
for 6h;
|
65%
|
|
With
1-[(1-(cyano-?2-?ethoxy-?2-?oxoethylidenaminooxy)?dimethylamino-?morpholino)]-uronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine;
In
N,N-dimethyl-formamide;
at 0 - 20 ℃;
for 6h;
Inert atmosphere;
|
65%
|
|
With
benzotriazol-1-ol; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide;
In
N,N-dimethyl-formamide;
|
|
|
{2-[(4-fluorobenzyl)sulfanyl]-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl}acetic acid;
With
benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride;
In
dichloromethane;
for 0.75h;
N,N-diethyl-N'-(4'-trifluoromethylbiphenyl-4-ylmethyl)ethane-1,2-diamine;
In
dichloromethane;
for 4h;
|
-
-
1349902-21-1
C19 H17 FN4 O2 S
-
-
304694-40-4
N,N-diethyl-N'-(4'-trifluoromethylbiphenyl-4-ylmethyl)ethane-1,2-diamine
-
-
356057-34-6
N-[2-(diethylamino)ethyl]-2-(2-{[(4-fluorophenyl)methyl]thio}-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl)-N-{[4’-(trifluoromethyl)-4-biphenylyl]methyl}acetamide
| Conditions | Yield |
|---|---|
|
In
isobutyl methyl ether;
at 92 ℃;
Industry scale;
|
356057-34-6 Upstream products
-
304694-40-4
N,N-diethyl-N'-(4'-trifluoromethylbiphenyl-4-ylmethyl)ethane-1,2-diamine
-
356058-42-9
{2-[(4-fluorobenzyl)sulfanyl]-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl}acetic acid
-
611-10-9
2-ethoxycarbonyl-1-cyclopentanone
-
35563-27-0
2-mercapto-1,5,6,7-tetrahydro-cyclopentapyrimidin-4-one