CAS: 24237-54-5; Ethyl 2-Amino-6-Benzyl-4,5,6,7-Tetrahydrothieno[2,3-C]Pyridine-3-Carboxylate

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CAS号3612-20-2 N-苄基-4-哌啶酮 | CAS号105-56-6 氰乙酸乙酯

1,1-二甲基-4-氧代-哌啶鎓碘化物置于吗啉,Potassium Carbonate,Sulfur体系中,用 乙醇,水 用作溶剂,化学反应生成替诺立定
参考文献:新型手性2-氨基-4,5,6,7-四氢噻吩并[2,3-C]吡啶衍生物的合成和抗菌评价
标题:新型手性2-氨基-4,5,6,7-四氢噻吩并[2,3-C]吡啶衍生物的合成和抗菌评价
摘要:采用方便的一锅三组分法合成了新的 N-取代-2-氨基-4,5,6,7-四氢噻吩并[2,3-C]吡啶衍生物,其结构通过 1H-NMR 和单晶体 X 射线衍射分析.所有合成的化合物都在体外筛选了对革兰氏阳性菌(八角藻)和革兰氏阴性菌(大肠杆菌)的抗菌活性.在这项工作中,我们在四氢吡啶氮上引入了一个手性残基,这是迄今为止对该药效团研究较少的位置,以探索其作用.抗菌结果表明,合成的化合物仅对革兰氏阳性菌有活性,(R)-对映异构体显示出比 (S)-对映体更大的抗菌效力.
Doi:10.1002/cbdv.201900097

专利信息

专利号:WO-9837078-A1
优先权日:1997-02-20
标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-6136984-A
优先权日:1996-04-22
标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-8546532-B2
优先权日:2008-04-17
标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
发明人：BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.

专利号:US-2024287041-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
发明人：BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

专利号:AU-2022276509-A1
优先权日:2021-05-20
标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

专利号:US-9994558-B2
优先权日:2013-09-20
标题 :Multicyclic compounds and methods of using same
发明人：BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).