CAS: 557795-19-4; (Z)-N-(2-(Diethylamino)Ethyl)-5-((5-Fluoro-2-Oxoindolin-3-Ylidene)Methyl)-2,4-Dimethyl-1H-Pyrrole-3-Carboxamide

上下游产品

N,N-diethylethylenediamine 5-((Z)-(5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid 5-fluoroindol-2(3H)-one N-[2-(diethylamino)ethyl]-3-oxobutanamidesunitinib malate 5-(5-Fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid(2-diethylamino-ethyl)-amide

Sunitinib Mesylate置于sodium Hydroxide体系中,用 水 作为反应溶剂,以99.5%的收率获得产物舒尼替尼
参考文献: Processes For The Preparation Of 3-(Pyrrol-2-yl)Methylene)-2-Pyrrolones Using 2-Silyloxy-Pyrroles[fr] Procédés Pour La Préparation De 3-((Pyrrol-2-yl)Méthylène)-2-Pyrrolones à L'Aide De 2-Silyloxypyrroles
标题: Processes For The Preparation Of 3-(Pyrrol-2-yl)Methylene)-2-Pyrrolones Using 2-Silyloxy-Pyrroles[fr] Procédés Pour La Préparation De 3-((Pyrrol-2-yl)Méthylène)-2-Pyrrolones à L'Aide De 2-Silyloxypyrroles
摘要:本发明提供了用于合成替代3-(吡咯-2-基)亚甲基)-2-吡咯酮的合成过程,包括舒尼替尼.本发明还提供了一种结晶基本纯舒尼替尼l-苹果酸的过程.

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-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:US-12312325-B2
优先权日:2022-03-01
标 题:Methods and compounds useful in the synthesis of an AAK1 inhibitor
发明人：CHEN TAO; WU WENXUE; YAN JUN; ZENG XIANGLU; ZHAO MATTHEW MANGZHU
权利人:LEXICON PHARMACEUTICALS INC
摘要:Methods for the synthesis of (S)-1-((2′,6-bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine and salts thereof are disclosed, as well as compounds useful therein.

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-2024209029-A1
优先权日:2021-04-21
标题:Adiponectin glycopeptides and compositions and methods of use thereof
发明人：WANG YU; LI XUECHEN; XU AIMIN; WU HONGXIANG; ZHANG YIWEI; LI YUANXIN
权利人:UNIV HONG KONG
摘要:An improved method for the chemical synthesis of glycosylated peptides has been developed. The method uses stereoselective glycan synthesis and chemical peptide ligation to produce glycopeptides at lower-cost and with higher efficiency/yield compared to conventional methods. In particular, a method for the large-scale, chemical synthesis of hydroxylated amino acid building blocks and glycosylated amino acids suitable for solid phase peptide synthesis (SPPS) are disclosed. SPPS-based methods using the glycosylated amino acids to chemically synthesize adiponectin-like peptides are also described. In vivo studies show that the adiponectin mimicking glycopeptides exhibit significant anticancer, anti-obesity and insulin sensitizing effects. Pharmaceutical compositions of the synthetic glycopeptides and methods of use thereof in treating diseases associated with deficient adiponectin are also described.