GDC-0084
1382979-44-3 Basic informationMore
- Product Name:GDC-0084
- Synonyms: GDC-0084 5-[8,9-Dihydro-6,6-dimethyl-4-(4-morpholinyl)-6H-[1,4]oxazino[4,3-e]purin-2-yl]-2-pyrimidinamine 5-(6,6-dimethyl-4-morpholino-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl)pyrimidin-2-amine 2-Pyrimidinamine, 5-[8,9-dihydro-6,6-dimethyl-4-(4-morpholinyl)-6H-[1,4]oxazino[4,3-e]purin-2-yl]- 5-[6,6-Dimethyl-4-(4-morpholinyl)-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl]-2-pyrimidinamine GDC-0084(RG7666) CS-2290 GDC-0084 (GDC0084
- CAS:1382979-44-3
- MF:C18H22N8O2
- MW:382.42
- EINECS:
- Mol File:1382979-44-3.mol
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).<br />
<img id="ProductImg1" src="https://www.chemicalbook.com/NewsImg/2019-03-08/20193811585028710.png" /><br />
Genentech’s route to GDC‐0084 employing a pivotal Suzuki reaction.
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- Company Name:Shanghai SuperLan Chemcial Technique Centre
- Tel:021-2022843681 15618226720
- Products Intro:Product Name:GDC-0084
CAS:1382979-44-3
Purity:95% Package:1G,5G,10G,50G,100G,1KG More... - CB Index:58
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- Company Name:Chengdu Celes Technology Co., Ltd
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- Products Intro:Product Name:Paxalisib, GDC-0084, RG7666
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CAS:1382979-44-3
Purity:98% HPLC Package:5KG;1KG;100g;1g - CB Index:58
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- Company Name:Dalian Meilun Biotech Co., Ltd.
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CAS:1382979-44-3
Purity:>98%,PI3KmTOR Package:5MG;25MG; - CB Index:58
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