亚甲基环己烷置于1.) Rhcl3>3 Sodium Hydroxide,双氧水,儿萘酚硼烷体系中,化学反应生成环己甲醇 参考文献:Transition Metal Catalysis In Fluorous Media: Practical Application Of A New Immobilization Principle To Rhodium-Catalyzed Hydroboration 标题:Transition Metal Catalysis In Fluorous Media: Practical Application Of A New Immobilization Principle To Rhodium-Catalyzed Hydroboration 摘要: Doi:10.1002/anie.199716101
专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:US-2025002518-A1 优先权日:2023-06-16 标 题 :Synthesis of heteroarynes and use thereof 发明人:MATTMILLER ROBERTS COURTNEY COLLEEN; HUMKE JENNA NICOLE; QUINLIVAN ANSEL ANNABEL; BELLI ROMAN GIANCARLO; KARGBO SALLU SO; PLASEK ERIN ELIZABETH 权利人:UNIV MINNESOTA 摘要:Disclosed herein are heterocyclic arynes and methods for preparing the same. Heteroarynes such as 5-membered O- or N-heterocyclic arynes have been considered inaccessible due to ring strain associated with the triple bond. The methods described herein demonstrate that these arynes can be successfully prepared through the utility of pi-backbonding from a transition metal. Synthetic utility of this method has been demonstrated by the facile synthesis and functionalization of heterocycles using these heteroaryne building blocks.
专利号:US-2002127598-A1 优先权日:2000-03-27 标题 :Solution-phase combinatorial library synthesis and pharmaceutically active compounds produced thereby 发明人:ZHOU WENQIANG; UPENDRAN SATHYA; IYER RADHAKRISHNAN P 摘要:The invention provides methods for solution-phase synthesis of nucleotide-based compounds and new libraries of such compounds. Compounds of the invention are useful for a variety of therapeutic applications, including treatment of viral or bacterial infections and associated diseases and disorders.
专利号:US-6620796-B1 优先权日:1999-11-08 标题:Combinatorial library synthesis and pharmaceutically active compounds produced thereby 发明人:ZHOU WENQIANG; JIN YI; ROLAND ARLENE; IYER RADHAKRISHNAN 权利人:MICROLOGIX BIOTECH INC 摘要:The invention provides new methods for synthesis of nucleotide-based compounds and new libraries of such compounds. Compounds of the invention are useful for a variety of therapeutic applications, including treatment of viral or bacterial infections and associated diseases and disorders.
专利号:US-4978744-A 优先权日:1989-01-27 标题:Synthesis of dolastatin 10 发明人:PETTIT GEORGE R; SINGH SHEO B 权利人:UNIV ARIZONA 摘要:A complicated but extremely important scheme of synthesis has been developed for synthesizing, dolaisoleuine, dolaproine, dolaphenine and dolavaline from readily available starting materials such as Z-(S,S)isoleucine, S-phenylalaline, S-phenylalaninol, S-prolinol, S-mandelate, and S-valine. The requisite amino acids have been combined using several peptide coupling procedures to create pharmaceutically pure dolastatin 10.
专利号:US-2009081801-A1 优先权日:2007-08-15 标题:Process for synthesis of pyrrole derivative, an intermediate for atorvastatin 发明人:KANSAL VINOD KUMAR; CHAURASIA BRIJNATH P; PATEL HITESH K; RAO V GOVARDHAN; DAUND VAIBHAV S 权利人:KANSAL VINOD KUMAR; CHAURASIA BRIJNATH P; PATEL HITESH K; RAO V GOVARDHAN; DAUND VAIBHAV S 摘要:The present invention also relates to a novel impurity, (6-{2-[2-(6-{2-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-phenylcarbamoyl-pyrrol-1-yl]-ethyl}-2,2-dimethyl-[1,3]-dioxan-4-yl)-acetylamino]-ethyl}-2,2-dimethyl-[1,3]-dioxan-4-yl)-acetic acid tert-butyl ester, the compound of formula IV, having the following structure: n n n n n n n n n n The present invention also provides methods of preparing the compound of formula IV as well as methods of using the compound of formula IV as a reference marker and a reference standard. n The present invention also provides an improved process for preparing (4R,cis)-6-[2-[3-phenyl-4-(phenyl-carbamoyl)-2-(4-fluorophenyl)-5-(1-methyl-ethyl)-pyrrole-1-yl]-2,2-dimethyl-[1,3]dioxane-4-yl-acetic acid-tertiary butyl ester, the compound of formula I, said process comprising the step of condensing 4-fluoro-α-[2-methyl-1-oxopropyl]-γ-oxo-N,β-diphenylbenzene butanamide, the compound of formula III, with (4R,Cis)-1,1-dimethylethyl-6-(2-aminoethyl)-2,2-dimethyl-1,3-dioxane-4-acetate, the compound of formula II, in the presence of a catalytic amount of an acid in the presence of a solvent system, preferably a binary solvent system, to obtain the desired compound (4R,cis)-6-[2-[3-phenyl-4-(phenyl-carbamoyl)-2-(4-fluorophenyl)-5-(1-methyl-ethyl)-pyrrole-1-yl]-2,2-dimethyl-[1,3]dioxane-4-yl-acetic acid-tertiary butyl ester.
参考标题:An Expedient Route For The Reduction Of Carboxylic Acids To Alcohols Employing 1-Propanephosphonic Acid Cyclic Anhydride As Acid Activator 作者:G. Nagendra,C. Madhu,T.M. Vishwanatha,Vommina V. Sureshbabu |发布日期:2012.9 摘要:Method For The Synthesis Of Alcohols From The Corresponding Carboxylic Acids Is Described. Activation Of Carboxylic Acid With 1-Propanephosphonic Acid Cyclic Anhydride (T3P) And Subsequent Reduction Using Nabh4 Yield The Alcohol In Excellent Yields With Good Purity. Reduction Of Several Alkyl/aryl Carboxylic Acids And Nα-Protected Amino Acids/peptide Acids As Well As Nβ-Protected Amino Acids Was Successfully
合成参考文献
摘要:Zaidlewicz, M.; Krzemiński, M. P.; Dzieleńdziak, A., Science of Synthesis, (2009) 48, 366. 摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 803. 摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 15. 摘要:Campagne, J. M.; Leclerc, E., Science of Synthesis Knowledge Updates, (2020) 2, 154. 摘要:Scammells, P. J., Science of Synthesis Knowledge Updates, (2013) 2, 445.