CAS: 1032900-25-6; 5-Chloro-N2-(2-Isopropoxy-5-Methyl-4-(Piperidin-4-yl)Phenyl)-N4-(2-(Isopropylsulfonyl)Phenyl)Pyrimidine-2,4-Diamine

上下游产品

2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(propane-2-sulfonyl)phenyl)pyrimidine-2,4-diamine dihydr°Chloride5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(propane-2-sulfonyl)phenyl)pyrimidine-2,4-diamine dihydr°Chloride 2-chloro-N-(2-(isopropylsulfonyl)phenyl)-5-methyl-pyrimidin-4-amine 4-(4-amino-5-isopropoxy-2-methylphenyl)-piperidine-1-carboxylic acid tert-butyl ester 4-(4-{5-chloro-4-[2-(propane-2-sulfonyl)phenylamino]pyrimidin-2-ylamino}-5-isopropoxy-2-methylphenyl)piperidine-1-carboxylic acid tert-butyl ester

Ceritinib Intermediate置于盐酸,Sodium Tetrahydroborate,氢气,钯体系中,用 甲醇,乙醇,水,异丙醇,乙腈 用作溶剂,20.0~50.0 °C,354.66 Kpa 条件下,反应 99.5H,反应生成色瑞替尼
参考文献:色瑞替尼中间体及其制备方法和应用
标题:色瑞替尼中间体及其制备方法和应用
摘要:本发明公开一种色瑞替尼中间体及其制备方法和应用.本发明的色瑞替尼中间体,结构如式i所示,R和r2的定义如说明书和权利要求书所示.色瑞替尼中间体由式1化合物与苄卤类化合物进行取代反应,再经还原制得.式i化合物进一步催化氢化还原硝基,脱除氨基保护后,与式ⅲ化合物在酸性条件下反应,得到色瑞替尼.本发明的方法,原料价廉易得,不需要特殊设备,生产成本大为降低,适合工业化应用.

专利信息

专利号:WO-2022146324-A1
优先权日:2020-12-29
标 题 :Synthesis of pyrimidine-4(lh)-one derivatives from new hydrazineylidene
发明人：SARIPINAR EMIN; BURCU HILAL JANSET; KEKEÇMUHAMMED HÃœSEYIN; TAPERA MICHAEL
权利人:T C ERCIYES UENIVERSITESI
摘要:This invention relates to the synthesis of pyrimidine-4 (1H)-one derivatives from Meldrum's acid, carbonyl compounds (aldehyde/ketone), and guanylhydrazone derivatives and tautomers, enantiomers, and salts thereof.

专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:US-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

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-2018140724-A1
优先权日:2015-05-27
标 题:Tumor Deliverable Iron and Protein Synthesis Inhibitors as a New Class of Drugs for the Diagnosis and Treatment of Cancer
发明人：DENG CHANGCHUN; LIPSTEIN MARK; O'CONNOR OWEN A
权利人:DENG CHANGCHUN; LIPSTEIN MARK; OCONNOR OWEN A; UNIV COLUMBIA
摘要:Tumor deliverable iron (TDI) drugs and pharmaceutical compositions and kits comprising them are provided and methods for delivering iron to tumors specifically, either intracellularly or extracellularly. As a result, TDI drugs are useful as a sensitizer for radiation therapy, radio-diagnosis, and chemotherapy, and are of interest. In other embodiments, tumor deliverable protein synthesis inhibitors (TDPSI) are provided and can be delivered to tumors, but not normal cells. These TDPSI drugs and pharmaceutical compositions and kits comprising them are useful for their treatment of cancer, either alone or in combination with other active anti-cancer drugs.

专利号:US-2022118123-A1
优先权日:2019-02-22
标 题 :Combination of ar antagonists and targeted thorium conjugates
发明人：HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
权利人:BAYER AG; BAYER AS
摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.