CAS: 1110813-31-4; (E)-N-(4-((3-Chloro-4-Fluorophenyl)Amino)-7-Methoxyquinazolin-6-yl)-4-(Piperidin-1-yl)But-2-Enamide

上下游产品

3-chloro-4-fluorophenylamine N'-(2-cyano-5-methoxy-4-nitrophenyl)-N,N-dimethylmethanimidamide 4-methoxyanthranilic acid

N-(3-氯-4-氟苯基)-7-氟-6-硝基-4-喹唑啉胺置于iron(III) Chloride,氯化亚砜,Hydrazine Hydrate,甲烷,Sodium Hydroxide体系中,用 四氢呋喃,N-甲基吡咯烷酮 用作溶剂,化学反应生成达克替尼
参考文献:一种达可替尼的制备方法
标题:一种达可替尼的制备方法
摘要:本发明公开了一种达可替尼的制备方法,其包括以下步骤:(N‑(3‑氯‑4‑氟苯基)‑7‑氟‑6‑硝基‑4‑喹唑啉胺)在碱/甲醇体系发生甲氧化反应,得化合物02(N‑(3‑氯‑4‑氟苯基)‑7‑甲氧基‑6‑硝基喹唑啉‑4‑胺);化合物02和水合肼发生还原反应,得化合物03(N‑(3‑氯‑4‑氟苯基)‑7‑甲氧基‑6‑氨基喹唑啉‑4‑胺);化合物03与酰氯化的化合物11((2E)‑4‑(1‑哌啶基)‑2‑丁烯酸盐酸盐)在n‑甲基吡咯烷酮溶剂中进行缩合反应得到粗品,再在乙醇水溶液中精制得到达可替尼.本发明的上述制备方法避免使用大量溶剂作为反应溶剂,从而做到尽量减少废液的产生,对环境更为友好;原料易得,安全,路线整体收率高,纯度高,能够有效的避免原料及催化剂难得和收率不高的弊端,有利于实现工业化,降低了生成成本.

专利信息

专利号:WO-2025128098-A1
优先权日:2023-12-13
标 题 :Solid oral dosage forms, kits, and methods of using the same
发明人：LI YING; LANGER ROBERT; TRAVERSO CARLO
权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

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-2023098592-A1
优先权日:2021-11-30
标题:Preparation method for carbon-loaded iron-based catalyst and use thereof in synthesis of intermediates of anti-cancer inhibitors

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-12180228-B2
优先权日:2019-06-05
标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
发明人：MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.