α-Methylmercaptopropionamidine置于硫酸体系中,化学反应生成1-甲基硫代-2-丙酮 参考文献:Kirrmann,A. Et Al.,Comptes Rendus Hebdomadaires Des Seances De L'Academie Des Sciences,1962,Vol. 255,P. 728-730 标题:Kirrmann,A. Et Al.,Comptes Rendus Hebdomadaires Des Seances De L'Academie Des Sciences,1962,Vol. 255,P. 728-730
专利号:US-2006257560-A1 优先权日:2004-12-30 标 题 :Polymer surfaces for insitu synthesis of polymer arrays 发明人:BARONE ANTHONY D; LI HANDONG; MCGALL GLENN H 权利人:AFFYMETRIX INC 摘要:In one aspect of the present invention polymers are used to create films providing three-dimensional array substrates. The films were stable and presented good hydroxyl group numbers as compared with arrays without polymer films. It is an object of the present invention that three dimensional arrays substrates provide a means to obtain higher density polymer arrays.
专利号:US-3901899-A 优先权日:1973-04-27 标题 :Synthesis of indoles from anilines and intermediates therein 发明人:GASSMAN PAUL G 权利人:UNIV OHIO STATE RES FOUND 摘要:Preparing indoles and intermediates therefor by reacting an Nhaloaniline with a Beta -carbonylic hydrocarbon sulfide to form an azasulfonium halide, reacting the azasulfonium halide with a strong base to form a thio-ether indole derivative, and then reducing the thio-ether indole, e.g. with Raney nickel, to form the indole compound. When an acetal or ketal of the Beta carbonyl hydrocarbon sulfide is used, the azasulfonium salt is treated with a base, and then with an acid to form the thio-ether indole derivative. When an Alpha -ethyl- Beta -carbonylic hydrocarbon sulfide is used, the resulting azosulfonium salt reacts with strong base to form a thio-ether indolenine derivative, which on reduction with Raney nickel or complex metal hydrides yields 3-substituted indoles. The aniline may be an aminopyridine to form an aza-indole compound in the process. The azasulfonium salts and thio-ether indole or thio-ether indolenine derivatives can be isolated and recovered from their respective reaction mixtures. The thio-ether-indole and thio-ether indolenine derivatives are useful as intermediates to make the indoles without the thio-ether group. The indoles are known compounds having a wide variety of uses, e.g., in making perfumes, dyes, amino acids, pharmaceuticals, agricultural chemicals and the like.
专利号:EP-0051792-A1 优先权日:1980-11-08 标 题 :Derivatives of hydroxamic-acid esters, process for their preparation and their use as herbicides 发明人:FUEHRER WOLFGANG DR; STETTER JOERG DR; EUE LUDWIG DR; SCHMIDT ROBERT RUDOLF DR 权利人:BAYER AG 摘要:Hydroxamic acid derivatives of the formula in which Y represents oxygen or sulfur, R¹ represents hydrogen, alkyl or alkoxy, R² represents hydrogen, alkyl, alkoxy or halogen, R³ represents hydrogen, alkyl, alkoxy or halogen, R < 4> represents hydrogen or alkyl, R <5> represents alkyl, alkenyl, alkynyl or alkoxyalkyl, R <6> represents hydrogen, alkyl, alkenyl, alkynyl or alkoxyalkyl or R <4> and R <5> together represent one Alkylene chain, or R 5 and R 6 together represent an alkylene chain, provided Y is oxygen and Z is halogen, a process for their preparation and their use as herbicides. N-phenylglycine derivatives of the formula in which Y, R¹, R², R³, R <4>, R <5> and R <6> have the meanings given above, several processes for their preparation and their use as intermediates for the synthesis of the substances of formula (I).
专利号:US-3992392-A 优先权日:1973-04-27 标题:Synthesis of indoles from anilines and intermediates therein 发明人:GASSMAN PAUL G 权利人:UNIV OHIO STATE RES FOUND 摘要:Preparing indoles and intermediates therefor by reacting an N-haloaniline with a β-carbonylic hydrocarbon sulfide to form an azasulfonium halide, reacting the azasulfonium halide with a strong base to form a thio-ether indole derivative, and then reducing the thio-ether indole, e.g. with Raney nickel, to form the indole compound. When an acetal or ketal of the β-carbonyl hydrocarbon sulfide is used, the azasulfonium salt is treated with a base, and then with an acid to form the thio-ether indole derivative. When an α-ethyl-β -carbonylic hydrocarbon sulfide is used, the resulting azosulfonium salt reacts with strong base to form a thio-ether indolenine derivative, which on reduction with Raney nickel or complex metal hydrides yields 3-substituted indoles. The aniline may be an aminopyridine to form an aza-indole compound in the process. The azasulfonium salts and thio-ether indole or thio-ether indolenine derivatives can be isolated and recovered from their respective reaction mixtures. The thio-ether-indole and thio-ether indolenine derivatives are useful as intermediates to make the indoles without the thio-ether group. The indoles are known compounds having a wide variety of uses, e.g., in making perfumes, dyes, amino acids, pharmaceuticals, agricultural chemicals and the like.
专利号:US-8927485-B2 优先权日:2010-02-18 标题:Site-specific modification of proteins through chemical modification enabling protein conjugates, protein dimer formation, and stapled peptides 发明人:KRANTZ ALEXANDER; YU PENG 权利人:KRANTZ ALEXANDER; YU PENG; ADVANCED PROTEOME THERAPEUTICS INC 摘要:The present invention generally provides methods for the site-specific modification of peptides, polypeptides, and proteins, e.g., granulocyte macrophage colony-stimulating factor, human superoxide dismutase, annexin, leptin, antibodies and the like, cytokines and chemokines, at their N-termini and at sites at which unnatural aminoacids have been introduced along the protein framework. The modifications described herein can be used for the synthesis and application of the adducts in radio-labeling, molecular imaging and protein therapeutic applications, and the treatment of disorders such as rheumatoid arthritis, lupus erythematosus, psoriasis, multiple sclerosis, type-1 diabetes, Crohn's disease, and systemic sclerosis, Alzheimer disease, cancer, liver disease (e.g., alcoholic liver disease), and cachexia.
专利号:US-9090629-B2 优先权日:2010-11-03 标题:Cytotoxic agents comprising new ansamitocin derivatives 发明人:CHARI RAVI V J; WIDDISON WAYNE C; WILHELM SHARON D 权利人:CHARI RAVI V J; WIDDISON WAYNE C; WILHELM SHARON D; IMMUNOGEN INC 摘要:New ansamitocin derivatives bearing a linking group are disclosed. Also disclosed are methods for the synthesis of these new ansamitocin derivatives and methods for their linkage to cell-binding agents. The ansamitocin derivative-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.
参考标题:Asymmetric Organocatalytic Direct Aldol Reactions Of Ketones With α-Keto Acids And Their Application To The Synthesis Of 2-Hydroxy-γ-Butyrolactones 作者:Xiao-Ying Xu,Zhuo Tang,Yan-Zhao Wang,Shi-Wei Luo,Lin-Feng Cun,Liu-Zhu Gong |发布日期:2007.12.1 摘要:Of Organocatalysts For The Asymmetric Direct Aldol Reactions Of Ketones With α-Keto Acids Were Designed On The Basis Of Molecular Recognition And Prepared From Proline And Aminopyridines. The Organic Molecule 8E, Derived From Proline And 6-Methyl-2-Amino Pyridine, Was The Best Catalyst, Affording Excellent Enantioselectivities (Up To 98% Ee) For The Direct Aldol Reactions Of Acetone Or 2-Butanone With
合成参考文献
摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 35. 摘要:Khartulyari, A.; Maier, M. E., Science of Synthesis Knowledge Updates, (2010) 3, 60. 摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 1006. 摘要:Clapés, P., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 82. 摘要:Grogan, G., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 3, 290.