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Darapladib

  • CAS No.: 356057-34-6
  • Purity: 99%
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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

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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

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Page/Page column 41; 42, (2016/05/11)

Pyrimidone compounds of formula (I): are...

PROCESSES FOR THE PREPARATION OF DARAPLADIB AND ITS INTERMEDIATES

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Page/Page column 19; 20, (2015/06/25)

The present invention provides a process...

356057-34-6 Process route

N,N-diethyl-N'-(4'-trifluoromethylbiphenyl-4-ylmethyl)ethane-1,2-diamine
304694-40-4

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
356058-42-9

{2-[(4-fluorobenzyl)sulfanyl]-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl}acetic acid

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
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
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;
C<sub>19</sub>H<sub>17</sub>FN<sub>4</sub>O<sub>2</sub>S
1349902-21-1

C19 H17 FN4 O2 S

N,N-diethyl-N'-(4'-trifluoromethylbiphenyl-4-ylmethyl)ethane-1,2-diamine
304694-40-4

N,N-diethyl-N'-(4'-trifluoromethylbiphenyl-4-ylmethyl)ethane-1,2-diamine

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
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
Conditions Yield
In isobutyl methyl ether; at 92 ℃; Industry scale;

356057-34-6 Upstream products

  • 304694-40-4
    304694-40-4

    N,N-diethyl-N'-(4'-trifluoromethylbiphenyl-4-ylmethyl)ethane-1,2-diamine

  • 356058-42-9
    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
    611-10-9

    2-ethoxycarbonyl-1-cyclopentanone

  • 35563-27-0
    35563-27-0

    2-mercapto-1,5,6,7-tetrahydro-cyclopentapyrimidin-4-one

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