CAS: 936091-26-8; N-(Tert-Butyl)-3-((5-Methyl-2-((4-(2-(Pyrrolidin-1-yl)Ethoxy)Phenyl)Amino)Pyrimidin-4-yl)Amino)Benzenesulfonamide

上下游产品

N-(tert-butyl)-3-((2-chloro-5-methylpyrimidin-4-yl)amino)benzenesulfonamide 4-(2-pyrrolidinoethoxy)aniline 3-bromo-(N-tert-butyl)benzenesulfonamide 2-chloro-4-amino-5-methylpyrimidine

3-氨基苯磺酰氟置于盐酸,1,1,3,3-四甲基二硅氧烷,1-羟基苯并三唑,N,N-二异丙基乙胺,Sodium Hydroxide体系中,用 甲醇,水,二甲基亚砜,异丙醇 作为反应溶剂,化学反应 72.5H,反应生成 N-(1,1-二甲基乙基)-3-[[5-甲基-2-[[4-[2-(1-吡咯烷基)乙氧基]苯基]氨基]-4-嘧啶基]氨基]苯磺酰胺
参考文献:磺酰氟和氟代硫酸盐的广谱催化酰胺化**
标题:磺酰氟和氟代硫酸盐的广谱催化酰胺化**
摘要:已经开发了一种广谱催化方法,用于合成磺酰胺和氨基磺酸盐.通过催化量的1-羟基苯并三唑(hobt)和硅添加剂的结合活化,磺酰氟和氟代硫酸盐的酰胺化反应顺利进行,通常获得优异的收率(87-99%).值得注意的是,该协议对于空间受阻的底物特别有效.催化剂的负载量通常很低,而金刚烷衍生物的十克级合成仅需要0.02 Mol%的催化剂.此外,通过关键中间体磺酰氟13合成市售药物fedratinib,已证明了该方法在药物化学中的潜力..由于大量的胺是可商购的,因此该途径提供了进入fedratinib类似物进行生物学筛选的简便途径.
DOI:10.1002/anie.202013976

专利信息

专利号:WO-2022269384-A1
优先权日:2021-06-24
标 题 :A process for the direct synthesis of fedratinib intermediate
发明人：DESAI ASIM HEMANTBHAI; PATIL SANJAY NIMBAJI; RADADIYA VAIBHAV GOVINDBHAI; DESAI JIGNASU THAKORBHAI; DUBEY RAJEEV RAMCHANDRA; CHOUBEY Ajit Kumar
权利人:AMI ORGANICS LTD
摘要:The present disclosure relates to a process for the direct synthesis of Fedratinib intermediate. Particularly, the present disclosure relates to a process for the direct synthesis of 3-amino-N- (tert-butyl)benzene sulfonamide. The process of the present disclosure has various advantages such as convenient operation conditions, time-saving process, easy purification, low operation costs, good yield and efficiency hence the process is industrially feasible. The use of non-toxic, inexpensive and easily available reagents, in the process of the present disclosure, makes the process cost-efficient economic and environmental friendly.

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人：ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

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-2025250277-A1
优先权日:2015-10-16
标 题 :PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF
发明人：ALLIAN AYMAN; JAYANTH JAYANTHY; MOHAMED MOHAMED-ESLAM F; MULHERN MATHEW M; NORDSTROM FREDRIK LARS; OTHMAN AHMED A; ROZEMA MICHAEL J; BHAGAVATULA LAKSHMI; MARROUM PATRICK J; MAYER PETER T; SHEIKH AHMAD Y; BORCHARDT THOMAS B; KLÃœNDER BEN; CAMP HEIDI S; PADLEY ROBERT J; VOSS JEFFREY W; PANGAN AILEEN L
权利人:ABBVIE INC
摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl) pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and vasculitis), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating giant cell arteritis (GCA).

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.