CAS: 186692-46-6; (R)-2-((6-(Benzylamino)-9-Isopropyl-9H-Purin-2-yl)Amino)Butan-1-Ol

上下游产品

(2R)-2-aminobutan-1-ol 2-chloro-6-phenylmethylamino-9-iso-propylpurine 6-benzyl-2-chloroadenineN6-benzyl-2-chloroadenine N-benzyl-2-fluoro-9H-purin-6-amine(2R)-2-[[6-benzylamino-9-isopropyl-9H-purin-2-yl]amino]butyl 4-(nitrooxy)-butanoate

📜2-氟-6-氯嘌呤置于potassium Carbonate,N,N-二异丙基乙胺体系中,用 2,4-滴二甲胺盐,二甲基亚砜,正丁醇 用作溶剂,化学反应 115.5H,反应生成[(1S)-1-氰基-2-甲基丙基]氨基甲酸苄酯
参考文献:Design,Synthesis And Biological Evaluation Of 6-Pyridylmethylaminopurines As Cdk Inhibitors
标题:Design,Synthesis And Biological Evaluation Of 6-Pyridylmethylaminopurines As Cdk Inhibitors
摘要:The Cyclin-Dependent Kinase (Cdk) Inhibitor Seliciclib (1,Cyc202) Is In Phase Ii Clinical Development For The Treatment Of Cancer. Here We Describe The Synthesis Of Novel Purines With Greater Solubility,Lower Metabolic Clearance,And Enhanced Potency Versus Cdks. These Compounds Exhibit Novel Selectivity Profiles Versus Cdk Isoforms. Compound Alpha Sbr-21 Inhibits Cdk2/cyclin E With Ic(50) = 30 Nm,Cdk7-Cyclin H With Ic(50) = 1.3 Mu M,And Cdk9-Cyclint With Ic(50) = 0.11 Mu M; It (Cct68127) Inhibits Growth Of Hct116 Colon Cancer Cells In Vitro With Gi(50) = 0.7 Mu M; And Shows Antitumour Activity When Dosed P.O. At 50 Mg/kg To Mice Bearing Hct116 Solid Human Tumour Xenografts. (C) 2011 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2011.08.051

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

专利号:US-8828984-B2
优先权日:2012-11-19
标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection
发明人：CHE CHI MING; ZOU TAOTAO
权利人:UNIV HONG KONG; UNIV HONG KONG
摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.

专利号:US-10577387-B1
优先权日:2018-08-09
标题 :Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment
发明人：CHE CHI MING; Fung Sin Ki; Chen tian feng
权利人:UNIV HONG KONG
摘要:Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.