CAS: 1703793-34-3; (S)-1-(4-Fluorophenyl)-1-(2-(4-(6-(1-Methyl-1H-Pyrazol-4-yl)Pyrrolo[2,1-F][1,2,4]Triazin-4-yl)Piperazin-1-yl)Pyrimidin-5-yl)Ethan-1-Amine

N-P-Toluenesulfonyl-4-Fluoroacetophenone Amine置于甲醇,Bis[(2,3,5,6-η)-(1R,4R)-2,5-2,5-Bis(4-Trifluoromethylphenyl)Bicyclo[2.2.2]octane-2-Diene]Bis-μ-Rhodium Chloride,Potassium Carbonate,苯硫酚,N,N-二异丙基乙胺体系中,用 1,4-二氧六环,N,N-二甲基甲酰胺 用作溶剂,化学反应 48.5H,反应生成阿泊替尼
参考文献:阿普替尼中间体的制备方法
标题:阿普替尼中间体的制备方法
摘要:本发明揭示了一种阿普替尼(Avapritinib)中间体(S)‑1‑(4‑氟苯基)‑1‑[2‑(哌嗪‑1‑基)嘧啶‑5‑基]乙胺的制备方法,其步骤包括:以4‑氟苯乙酮为起始原料,依次经过亚胺化反应,有机金属催化下的加成反应和水解反应生成目标化合物(S)‑1‑(4‑氟苯基)‑1‑[2‑(哌嗪‑1‑基)嘧啶‑5‑基]乙胺.该制备方法工艺简洁,条件温和,安全环保,为阿普替尼的工业化生产提供了一条新的途径.

专利信息

专利号:WO-2025038767-A1
优先权日:2023-08-14
标 题:Cell-free synthesis platform for synthetically dimierized, clickable fragment antigen-binding (fab) fragments
发明人：THAMES ARIEL; RISCHE CLAYTON; JEWETT MICHAEL; BOCHNER BRUCE
权利人:UNIV NORTHWESTERN
摘要:Disclosed are components, systems, methods, and kits for synthesis of diamerized, clickable antigen binding fragments, such as Fab fragments, and uses thereof. The components, systems, methods, and kits disclosed herein utilize cell-free protein synthesis (CFPS) systems and methods to produce clickable antigen binding fragments.

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-2024208898-A1
优先权日:2021-03-25
标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents
发明人：KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T
权利人:DANA FARBER CANCER INST INC
摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.

专利号:WO-2024245115-A1
优先权日:2023-05-31
标 题:Preparation method for pyrrolotriazine compound
发明人：GUO SONGJING; TU GUOLIANG; JIN YEHUA; ZHU WEI; MENG YANHUA
权利人:LINHAI HUANAN CHEMICAL CO LTD; ZHEJIANG HUAHAI PHARM CO LTD
摘要:The present invention relates to the technical field of drug synthesis. A first aspect of the present invention provides a preparation method for a monochloramine organic solution. Another aspect of the present invention provides a use of the preparation method in amination reaction or in preparation of compound 4. The other aspect of the present invention provides a preparation method for compound 4. The present invention also provides preparation methods for compounds 2 and 3. The present invention has a short entire process route, low costs, less generation of three wastes, simple post-treatment, high yield and excellent product quality, and is suitable for industrial production.

专利号:WO-2025137620-A1
优先权日:2023-12-21
标题:Methods for high quality and high accuracy methylation sequencing
发明人：KENNEDY ANDREW
权利人:GUARDANT HEALTH INC
摘要:Provided herein are methods and compositions for calibrating one or more base calling metrics in a sequencing by synthesis reaction, and for calling at least a portion of nucleobases in a converted region of a DNA molecule using the one or more calibrated base calling metrics. Provided herein are also methods for determining the likelihood that a subject has a disease or condition, such as cancer.

专利号:JP-2024512568-A
优先权日:2021-03-25
标 题:Enamine N-oxide: synthesis and application of hypoxia-responsive prodrugs and contrast agents