CAS: 610798-31-7; N-(3-Ethynylphenyl)-7,8,10,11,13,14-Hexahydro-[1,4,7,10]Tetraoxacyclododecino[2,3-G]Quinazolin-4-Amine

上下游产品

trimethylsilylacetylene 14H17NO8C14H17NO8 3,4-dihydroxybenzoic acid methyl ester 14H19NO6C14H19NO6

2-氨基-4,5-二氟苯甲酸置于氨,Sodium Hydride,Potassium Carbonate,Copper(I) Bromide,三氯氧磷体系中,用 四氢呋喃,甲醇,二氯甲烷,1,2-二氯乙烷 作为反应溶剂,化学反应 68.0H,反应生成 埃克替尼
参考文献:一种埃克替尼的制备方法
标题:一种埃克替尼的制备方法
摘要:一种埃克替尼的制备方法,步骤:将2‑氨基‑4,5‑二氟苯甲酸与酰胺化试剂的溶液充分混合,加入催化剂,进行酰胺化反应;将得到的2‑氨基‑4,5‑二氟苯甲酰胺与环化试剂溶于溶剂中,在高温下进行环化反应;将得到的6,7‑二氟‑3,4‑二氢喹唑啉‑4‑酮与氯化试剂在溶剂体系中进行氯化反应;将得到的4‑氯‑6,7‑二氟喹唑啉与3‑乙炔基苯胺在碱试剂和溶剂体系中进行缩合反应;将得到的4‑[(3‑乙炔基苯基)氨基]‑6,7‑二氟喹唑啉与二缩三乙二醇在碱试剂和溶剂体系中进行醚化反应,得到埃克替尼.杂质较少,可控,可直接进行下一步反应,简化操作,每一步都能获得非常好的收率;简化工艺流程,保障安全与环保.

专利信息

专利号:US-9359370-B2
优先权日:2008-07-08
标题 :Icotinib hydrochloride, synthesis, crystalline forms, pharmaceutical compositions, and uses thereof
发明人：WANG YINXIANG; XIE GUOJIAN; DING LIEMING; TAN FENLAI; HU YUNYAN; HE WEI; HAN BIN; LONG WEI; LIU YONG; Ai haima; DAVIS CHARLES; ZHANG DON
权利人:BETA PHARMA INC
摘要:The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.

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:US-2022259212-A1
优先权日:2019-07-11
标题:Inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase
发明人：BOSS CHRISTOPH; CREN SYLVAINE; KIMMERLIN THIERRY; LOTZ-JENNE CARINA; POTHIER JULIEN; TIDTEN-LUKSCH NAOMI
权利人:IDORSIA PHARMACEUTICALS LTD
摘要:The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in the treatment of inter alia cancer is disclosed.

专利号:US-11406709-B2
优先权日:2014-09-15
标 题 :Therapeutic and research application of PDCL3
发明人：RAHIMI NADER
权利人:UNIV BOSTON
摘要:Described herein are novel compositions comprising, for example, PDCL3 polypeptides having VEGFR-2 inhibitory activity, inhibitory PDCL3 antibodies and PDCL3-binding fragments thereof, or PDCL3 inhibitory nucleic acid molecules, and methods of their use in anti-angiogenesis and anti-tumor proliferation and invasiveness therapies, such as the treatment of cancer, as well as the treatment of those vascular diseases where pathological angiogenesis plays a role, such as in carotid artery disease, macular degeneration, and plaque neovascularization. Also described herein are novel compositions comprising engineered PDCL3 polypeptides having enhanced chaperone activity, recombinant cells comprising such engineered PDCL3 polypeptides having enhanced chaperone activity, and methods thereof for therapeutic protein production and in vitro protein synthesis.

专利号:US-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人：EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

专利号:US-10272065-B2
优先权日:2013-01-14
标题 :Gem-difluorinated C-glycoside compounds as anti-cancer agents
发明人：SLILATY STEVE N
权利人:ADVANOMICS CORP; BENOIT & COTE
摘要:The present document describes a synthesis of a class of gem-difluorinated C-glycoside compounds derived from podophyllotoxin, which may be used, but not exclusively, in oncology for the treatment of cancer. More particularly, the podophyllotoxin gem-difluorinated C-glycoconjugated derivatives display improved conformational and chemical stability, and improved cytotoxicity exhibited against drug-resistant cancer cell lines.