对氯苯甲腈置于氨,氢气体系中,用 甲醇 用作溶剂,60.0 °C,4.0 Mpa 条件下,反应 18.0H,以91%的收率获得对氯苄胺 参考文献:稳定且可重复使用的镍基纳米颗粒,用于将腈类普遍和选择性氢化成胺 标题:稳定且可重复使用的镍基纳米颗粒,用于将腈类普遍和选择性氢化成胺 摘要:二氧化硅负载的超小 Ni 纳米颗粒允许在温和条件下将各种腈类普遍和选择性地氢化为伯胺.通过煅烧由 Ni( Ii ) 生成的模板材料)硝酸盐和胶体二氧化硅在空气下,随后在分子氢存在下还原,制备最佳催化剂.制备的负载型纳米颗粒稳定,使用方便,易于回收利用.最佳催化剂材料的适用性通过对超过 110 种不同的脂肪族和芳香族腈(包括功能化和工业相关底物)进行氢化来证明.具有挑战性的杂环腈,特别是氰基吡啶,以非常好的收率提供了相应的伯胺.所得胺可作为制备众多生命科学产品和聚合物的重要前体和中间体. Doi:10.1039/d2Sc02961H
专利信息
专利号:WO-2021260722-A1 优先权日:2020-06-21 标 题:Design, synthesis of novel oxyindole inhibitors of denv rna dependent rna polymerase 发明人:GUNDLA RAMBABU; ASTHANA SHAILENDRA; BHATTACHARYYA SANKAR; MADDIPATI VENKATANARAYANA CHOWDARY; MITTAL LOVIKA; KAUR JASKARAN; RAWAT YOGITA 权利人:TRANSLATIONAL HEALTH SCIENCE AND TECH INSTITUTE; GANDHI INSTITUTE OF TECH AND MANAGEMENT 摘要:The present invention is drawn to novel compounds of formula I, II and III, including any conformational isomeric form, salts and solvates for inhibition of DENV RNA dependent and RNA polymerase. The present invention also discloses a process of synthesis of the compounds, compositions comprising the said compounds and use of the compounds and treatment comprising the compounds of the present invention.
专利号:WO-0027627-A1 优先权日:1998-11-12 标题 :Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles 发明人:WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 权利人:LILLY CO ELI; WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 摘要:In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.
专利号:EP-0310950-B1 优先权日:1983-11-18 标题 :Quinoline intermediates for the synthesis of 1H-imidazo[4,5-c]quinolines and 1H-imidazo[4,5-c]quinolin-4-amimes 摘要:Compounds of the types (I) and (II) are disclosed, wherein each R5 is independently selected from the group consisting of alkyl of one to about four carbon atoms, alkoxy of one to about four carbon atoms and halogen, and n is an integer from 0 to 2, with the proviso that if n is 2, then said R5 substituents together contain no more than 6 carbon atoms; R6 is selected from the group consisting of hydroxyalkyl of one to about six carbon atoms and cyclohexylmethyl; and R7 is selected from the group consisting of alkyl of one to about four carbon atoms and hydrogen. These compounds may be used as intermediates for the synthesis of 1H-imidazo[4,5-c]quinoline derivatives.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-6228988-B1 优先权日:1995-02-24 标题:Synthesis of hydroxamic acid derivatives 发明人:FLOYD CHRISTOPHER DAVID; LEWIS CHRISTOPHER NORMAN 权利人:BRITISH BIOTECH PHARM 摘要:The present invention describes processes for preparing desired synthetic products that comprise a covalently bonded hydroxamic acid group -CONHOH by forming a mixture of a liquid reaction medium and a solid phase reaction product that carries a plurality of moieties of formula (A1) or (B1):where X is a residual, non-hydroxamate partial structure of the desired synthetic product, P1 is hydrogen or an amino-protecting group, P2 is hydrogen or a hydroxyl protecting group, and the bond designated (a) covalently links the moieties (A1) or (B1) to the residue of a solid substrate; by cleaving the bond designated (a) in the resultant mixture; and by separating the resultant liquid reaction phase from the resultant reaction solids to recover the desired synthetic product.
专利号:US-3553221-A 优先权日:1968-01-22 标 题:Certain intermediates for the production of beta-collidine 发明人:GUTZWILLER JUERG ALBERT WALTER; USKOKOVIC MILAN RADOJE 权利人:HOFFMANN LA ROCHE 摘要:THE PREPARATION OF B-COLLIDINE FROM METHYL VINYL KETONE AND AN AMINE SUCH AS, FOR EXAMPLE, BENZYLAMINE, THROUGH VARIOUS INTERMEDIATES, FOR EXAMPLE, 3-ACETYL-1BENZYL - 1,2,5,6, - TETRAHYDRO - 4 METHYLPYRIDINE, 3 ACETYL - 1,2,5,6 - TETRAHYDRO - 4 - METHYLPYRIDINE, 3ACETYL - 4 - METHYLPYRIDINE, 1 - BENZYL - 3 - (1 - HYDROXYETHYL) - 1,2,5,6 - TETRAHYDRO - 4 - METHYLPYRIDINE, 3-(1HYDROXYETHYL)-4-METHYLPYRIDINE AND 1-BENZYL-3-ETHYLENE1,2,3,6-TETRAHYDRO-4-METHYLPYRIDINE, IS DESCRIBED, B-COLLIDINE, I.E., 3-ETHYL-4-METHYLPYRIDINE, IS USEFUL IN THE SYNTHESIS OF, FOR EXAMPLE, DIHYDROQUINIDINE.
[参考文献]: Kenji Matsuno, Et Al. S-Benzylisothiourea Derivatives As Small-Molecule Inhibitors Of Indoleamine-2,3-Dioxygenase. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5126-9.
合成参考文献
摘要:Chciuk, T. V.; Flowers, R. A.; Flowers, R. A., Science of Synthesis Knowledge Updates, (2016) 2, 229. 摘要:Wu, X.-F., Science of Synthesis Knowledge Updates, (2014) 1, 339. 摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 72. 摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 22. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 98.