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GDC-0084

GDC-0084

CAS:
1382979-44-3
MF:
C18H22N8O2
MW:
382.42

Properties

Density 
1.60±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
insoluble in H2O; insoluble in EtOH; ≥2.83 mg/mL in DMSO with ultrasonic
form 
Solid
pka
2.62±0.40(Predicted)

Safety Information

Symbol(GHS) 

GHS07
Signal word 
Warning
Hazard statements 
H302-H315-H319-H335
Precautionary statements 
P261-P305+P351+P338

Use

Stumpf et al. at Genentech Inc. (Roche group) developed an efficient multikilogram process to synthesize the brain penetrant PI3K inhibitor, GDC‐0084, a potential drug candidate for the treatment of several brain cancers. An efficient Suzuki coupling reaction between a chloropyrimidine and an arylboronic ester using a palladium catalyst at low loading was reported. The optimized conditions were demonstrated on 6.75 kg of a chloropyrimidine intermediate, providing 7.49 kg of crude GDC‐0084 (94% yield, 99.4% HPLC purity). Using the commercially available XPhos Pd G2 catalyst, instead of the usual PdCl2(dppf)CH2Cl2 catalyst, it was possible to reduce the catalyst loading from 2 to 0.5 mol%. A final scavenging/recrystallization combination from Si‐Thiol (a solid‐supported resin) and acetic acid/water provided the crude GDC‐0084 with the required purity and polymorphic form (off‐white solid, 6.41 kg, 83% yield, 99.7% HPLC purity). Genentechs route to GDC‐0084 employing a pivotal Suzuki reaction.

0 India supplier list of "GDC-0084"

  • Product Name:GDC-0084
  • Products Intro:Brand:ajchemicals | Product Number:JDH-30600 | Purity:98+%
  • Company Type: Trader
  • Country/Region: New Delhi,INDIA
  • Product Name:GDC0084
  • Products Intro:Brand:clearsynth | Product Number:CS-T-78865
  • Company Type: Trader
  • Country/Region: Hyderabad,INDIA
  • Product Name:GDC-0084
  • Products Intro:Purity: 98% | Package: 10MG;50MG;100MG,1G,5G,10G.100G
  • Company Type: Reagent
  • Country/Region: CHINA
  • Product Name:GDC-0084
  • Products Intro:Purity: 98% | Package: 300mg | CustNote: BOC Sciences also provides custom synthesis services for GDC-0084.
  • Company Type: Trader
  • Country/Region: UNITED STATES
  • Product Name:5-(6,6-dimethyl-4-morpholino-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl)pyrimidin-2-amine
  • Products Intro:Purity: 98% | Package: 1g,5g,10g
  • Company Type: Trader
  • Country/Region: CHINA
  • Product Name:GDC-0084
  • Products Intro:Purity: 99% | Package: 5KG;1KG | CustNote: GDC-0084
  • Company Type: Trader
  • Country/Region: CHINA
  • Main Products: sarms
  • Product Name:GDC-0084
  • Products Intro:Purity: 0 | Package: 1g; 5g; 25g; 1kg; 5kg; 25kg | CustNote: 0
  • Company Type: Trader
  • Country/Region: CHINA
  • Main Products: Pharmaceutical intermediate
  • Product Name:Paxalisib (GDC-0084)
  • Products Intro:Purity: 99% | Package: $254.9/5mg;$408.9/10mg;$817.9/25mg;$1510.9/50mg;Bulk package | CustNote: 99%
  • Company Type: Trader
  • Country/Region: UNITED STATES
  • Main Products: Chemicals and BioChemicals,Materials Science,ligands acting on targets,Proteins,Antibodies
  • Product Name:GDC-0084
  • Products Intro:Purity: 0.98 | Package: 10G:100G
  • Company Type: Trader
  • Country/Region: CHINA
  • Main Products: MRTX1133,(cas:2055858-27-8)1,1′-Sulfinylbis[3,5-difluorobenzene,(cas:17220-38-1) 3,4-Diaminofurazane,Mirogabalin besylate,AK2292

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