CAS: 362-07-2; (8R,9S,13S,14S,17S)-2-Methoxy-13-Methyl-7,8,9,11,12,13,14,15,16,17-Decahydro-6H-Cyclopenta[a]Phenanthrene-3,17-Diol

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CAS号362-08-3 2-甲氧基雌素酮 | CAS号24381-12-2 2-iodoestradiol | CAS号124-41-4 甲醇钠 | CAS号15833-07-5 2-溴雌二醇 | CAS号627893-66-7 2-methoxyestrad... | CAS号50-28-2 雌二醇 | CAS号362-05-0 2-羟基-17β-雌二醇 | CAS号362-08-3 2-甲氧基雌素酮

3,17β-Bis(Benzyloxy)-2-Methoxyestra-1,3,5(10)-Triene置于palladium On Activated Charcoal 氢气体系中,用 四氢呋喃 用作溶剂,以11.5 Mg的收率获得2-甲氧基雌二醇
参考文献:Synthesis,Antitubulin And Antimitotic Activity,And Cytotoxicity Of Analogs Of 2-Methoxyestradiol,An Endogenous Mammalian Metabolite Of Estradiol That Inhibits Tubulin Polymerization By Binding To The Colchicine Binding Site
标题:Synthesis,Antitubulin And Antimitotic Activity,And Cytotoxicity Of Analogs Of 2-Methoxyestradiol,An Endogenous Mammalian Metabolite Of Estradiol That Inhibits Tubulin Polymerization By Binding To The Colchicine Binding Site
摘要:In Order To Define The Structural Parameters Associated With The Antitubulin Activity And Cytotoxicity Of 8-Methoxyestradiol,A Mammalian Metabolite Of Estradiol,An Array Of Analogs Was Synthesized And Evaluated. The Potencies Of The New Congeners As Inhibitors Of Tubulin Polymerization And Colchicine Binding Were Determined Using Tubulin Purified From Bovine Brain,And The Cytotoxicities Of The New Compounds Were Studied In A Variety Of Cancer Cell Cultures. Maximum Antitubulin Activity Was Observed In Estradiols Having Unbranched Chain Substituents At The 2-Position With Three Non-Hydrogen Atoms. 2-Ethoxyestradiol And 2-((E)-1-Propenyl)-Estradiol Were Substantially More Potent Than 2-Methoxyestradiol Itself. The Tubulin Polymerization Inhibitors In This Series Displayed Significantly Higher Cytotoxicities In The Mda-Mb-435 Breast Cancer Cell Line Than In The Other Cell Lines Studied. The Potencies Of The Analogs As Cytotoxic And Antimitotic Agents In Cancer Cell Cultures Correlated With Their Potencies As Inhibitors;Of Tubulin Polymerization,Supporting The Hypothesis That Inhibition Of Tubulin Polymerization Is The Mechanism Of The Cytotoxic Action Of 2-Methoxyestradiol And Its Congeners. Several Of The More Potent Analogs Were Tested In An Estrogen Receptor Binding Assay,And Their Affinities Relative To Estradiol Were Found To Be Very Low.
Doi:10.1021/jm00012A003

专利信息

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-6448419-B1
优先权日:2001-08-07
标题:Synthesis of 2-hydroxyestradiol derivatives
发明人：PAAREN HERBERT E; DUFF STEVEN R
权利人:TETRIONICS INC
摘要:Disclosed is a method of preparing 2-hydroxy-3,17β-estradiol derivatives wherein 3,17β-estradiol is reacted with an organolithium reagent and reacted with either a boron reagent or a silicon reagent to form either a 2-boronyl or a 2-silyl modified estradiol analog represented by the corresponding structural formulae: n R 1 and R 2 are each independently a hydroxyl protecting group. R 3 , R 4 and R 5 are selected from the group consisting of halogens, alkyl, aryl, hydroxy, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl.

专利号:US-6054598-A
优先权日:1997-03-13
标题 :Synthesis of 2-alkoxyestradiols
发明人：SACHDEVA YESH; RAM SIYA
权利人:PHARM ECO LAB INC
摘要:Disclosed is a method of preparing a compound represented by the following structural formula: The method comprises reacting bromine (Br2) and an aliphatic organic acid with a compound represented by the following structural formula: R1 and R2 are each independently a hydroxyl protecting group.

专利号:US-7935704-B2
优先权日:2003-08-01
标 题 :Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
发明人：PALLADINO MICHAEL A; LLOYD GEORGE KENNETH; HAYASHI YOSHIO; NICHOLSON BENJAMIN
权利人:NEREUS PHARMACEUTICALS INC
摘要:Compounds represented by the following structure (I) are disclosed: n nas are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ′, R 1 ″, R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.