GDC-0084 suppliers
GDC-0084
- CAS:
- 1382979-44-3
- MF:
- C18H22N8O2
- MW:
- 382.42
Suppliers by country/region
Company Type
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.
61 supplier list of "GDC-0084"
$1.00/ 1KG
- Product Name:5-[6,6-Dimethyl-4-(4-morpholinyl)-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl]-2-pyrimidinamine
- Products Intro:Purity: Min98% HPLC | Package: 1KG;1USD
- Company Type: Trader
- Country/Region: CHINA