GDC-0084 manufacturers and suppliers

GDC-0084 suppliers

GDC-0084

CAS:: 1382979-44-3

MF:: C18H22N8O2

MW:: 382.42

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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

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.

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