CAS: 503468-95-9; 8-(Dibenzo[b,D]Thiophen-4-yl)-2-Morpholino-4H-Chromen-4-One

上下游产品

2-Morpholin-4-Yl-4-Oxo-4H-Chromen-8-Yl Trifluoromethanesulfonate 351002-11-4

4-乙酰基吗啉置于四(三苯基膦)钯,三氟甲磺酸酐,Potassium Carbonate,Lithium Diisopropyl Amide体系中,用 四氢呋喃,1,4-二氧六环,正己烷,二氯甲烷 作为反应溶剂,化学反应 94.0H,反应生成 8-(4-二苯并噻吩基)-2-(4-吗啉基)-4H-1-苯并吡喃-4-酮
参考文献:Discovery Of Potent Chromen-4-One Inhibitors Of The Dna-Dependent Protein Kinase (Dna-Pk) Using A Small-Molecule Library Approach
标题:Discovery Of Potent Chromen-4-One Inhibitors Of The Dna-Dependent Protein Kinase (Dna-Pk) Using A Small-Molecule Library Approach
摘要:Structure-Activity Relationships For Inhibition Of Dna-Dependent Protein Kinase (Dna-Pk) Have Been Defined For Substituted Chromen-4-Ones. For The 2-Amino-Substituted Benzo[h]Chromen-4-Ones,A Morpholine Substituent At This Position Was Essential For Activity. Small Libraries Of 6-And 7-Alkoxy-Substituted Chromen-4-Ones Showed That A Number Of 7-Alkoxysubstituted Chromenones Displayed Improved Activity. Focused Libraries Incorporating 6-,7-,And 8-Aryl And Heteroaryl Substituents Were Prepared. In These Cases,6-And 7-Substitution Was Disfavored,Whereas 8-Substitution Was Largely Tolerated. Surprisingly,Two Compounds,2-N-Morpholino-8-Dibenzofuranyl-Chromen-4-One (Nu7427,32{38}) And The 2-N-Morpholino-8-Dibenzothiophenyl-Chromen-4-One (Nu7441,32{26}) Were Excellent Inhibitors (Ic50 Vs Dnapk = 40 And 13 Nm,Respectively). The Ring-Saturated Analogue 2-N-Morpholino-8-(6',7',8',9'-Tetrahydrodibenzothiophene)Chromen-4-One,36,Retained Potent Activity (Ic50 Vs Dna-Pk = 23 Nm). The Dibenzothiophene 32{38} Sensitized Hela Cells To Ionizing Radiation In Vitro,With Dose Modification Factors Of 2.5 At 10% Survival Being Observed At 0.5 Mu M. The Cytotoxicity Of The Topoisomerase Ii Inhibitor Etoposide Was Also Potentiated.
DOI:10.1021/jm050444B

专利信息

专利号:US-2009326223-A1
优先权日:2006-07-18
标题 :Synthesis of 2-amino-substituted 4-oxo-4h-chromen-8.yl-trifluoro-methanesulfonic acid esters
发明人：GRIFFIN ROGER JOHN; HARDCASTLE IAN ROBERT; DESAGE-EL MURR MARINE; RODRIGUEZ-ARISTEGUI SONSOLES; GOLDING BERNARD THOMAS
权利人:GRIFFIN ROGER JOHN; HARDCASTLE IAN ROBERT; DESAGE-EL MURR MARINE; RODRIGUEZ-ARISTEGUI SONSOLES; GOLDING BERNARD THOMAS
摘要:A method of synthesising a compound of formula (I): wherein R N1 and R N2 are independently selected from hydrogen, an optionally substituted C 1-7 alkyl group, C 3-20 heterocyclyl group, or C 5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; from a compound of formula (III): comprising the steps of: (a) removing the allyl group from the compound of formula (III) with appropriate reaction conditions to yield a compound of formula (II): and (b) reacting the compound of formula (II) with a triflating agent to yield a compound of formula (I).

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.

专利号:WO-2008009934-A1
优先权日:2006-07-18
标 题 :Synthesis of 2-amino-substituted 4-oxo-4h-chromen-8.yl-trifluoro-methanesulfonic acid esters