CAS: 98319-26-7; (4Ar,4Bs,6As,7S,9As,9Bs,11Ar)-N-(Tert-Butyl)-4A,6A-Dimethyl-2-Oxo-2,4A,4B,5,6,6A,7,8,9,9A,9B,10,11,11A-Tetradecahydro-1H-Indeno[5,4-F]Quinoline-7-Carboxamide

上下游产品

CAS号98319-24-5 二氢波斯卡 | CAS号684215-49-4 N-tert-butyl-2-... | CAS号103335-41-7 非那雄胺中间体 | CAS号94-13-3 对羟基苯甲酸丙酯 | CAS号99-76-3 尼泊金甲酯 | CAS号877080-59-6 4-aza-androst-5... | CAS号877080-58-5 4-aza-5-androst... | CAS号63-05-8 雄烯二酮 | CAS号6857-88-1 4-Nor-3,5-seco-...

二氢波斯卡置于bstfa,2,3-二氯-5,6-二氰基-1,4-苯醌体系中,化学反应生成 非那雄胺
参考文献:氮杂类固醇的结晶工程:在非那雄胺的开发中的应用
标题:氮杂类固醇的结晶工程:在非那雄胺的开发中的应用
摘要:开发了基于固溶体形成的新颖且稳健的结晶方法,用于非那雄胺的纯化.这是一种空前的方法,它描述了使用纯非那雄胺1纯化不同批次的被二氢非那雄苷2污染的非那雄胺1(不纯).
DOI:10.1021/op300142A

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:WO-2009034398-A1
优先权日:2007-09-11
标题:Process for the synthesis of 6-hydroxymethyl-l,4- androstadien-3.17-dione
发明人：HANTOS GABOR; HERINE BERTA MONIKA; TEGDES ANIKO; BARTHO ISTVAN; DEVENYI TAMAS; GALIK GYOERGY; PECSNE RAZSO AGNES; GANCSOS VALERIA; KOENCZOEL KALMAN; MAHO SANDOR
权利人:RICHTER GEDEON NYRT; HANTOS GABOR; HERINE BERTA MONIKA; TEGDES ANIKO; BARTHO ISTVAN; DEVENYI TAMAS; GALIK GYOERGY; PECSNE RAZSO AGNES; GANCSOS VALERIA; KOENCZOEL KALMAN; MAHO SANDOR
摘要:The invention relates to a novel process for the synthesis of 6-hydroxymethyl-l,4- androstadien-3,17-dione which means dehydrogenating 6-hydroxymethyl-4-androsten- 3,17-dione in the presence of a biocatalyst.

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

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.