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-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:US-6225341-B1 优先权日:1995-02-27 标 题:Compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; WILLIAMS MATTHEW A 权利人:GILEAD SCIENCES INC 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:US-3668220-A 优先权日:1967-10-13 标 题:Adamantane compounds 发明人:SZINAI STEPHEN S; LUNN WILLIAM H W 权利人:LILLY CO ELI 摘要:WHEREIN EACH G independently represents hydrogen or straightchain alkyl of from one to six, both inclusive, carbon atoms; G'' represents hydrogen or acetyl; R represents hydrogen or alkyl of from one to six, both inclusive, carbon atoms; R'' represents halo, alkoxy containing from one to six both inclusive, carbon atoms in the alkyl group, hydrogen or alkyl of from one to six, both inclusive, carbon atoms; each R'''' independently represents hydrogen or alkyl of from one to six, both inclusive, carbon atoms; each R'''''' independently represents hydrogen or alkyl of from one to six, both inclusive, carbon atoms or both R'''''' groups taken together represent oxo(-0); X represents halo; and each n independently represents an integer of from zero to one, both inclusive. The terms ''''halo'''' and ''''halide'''' are employed herein to designate occurrences of bromine, chlorine and iodine. The adamantane compounds of formula VII AND VIII are useful as agents to achieve a depressant action on the central nervous system of warm blooded animals. The adamantane compounds of formulas I, II, III, IV, V and VI are useful as intermediates in the synthesis of the compounds of formulas VII and VIII. The present invention is directed to adamantane compounds of the formula:
专利号:US-3859352-A 优先权日:1966-10-24 标题 :Adamantane compounds 发明人:SZINAI STEPHEN S; LUNN WILLIAM H W 权利人:LILLY CO ELI 摘要:The present invention is directed to adamantane compounds of the formulae: WHEREIN EACH G independently represents hydrogen or straightchain alkyl of from 1 to 6, both inclusive, carbon atoms; G'' represents hydrogen or acetyl; R represents hydrogen or alkyl of from 1 to 6, both inclusive, carbon atoms; R'' represents halo, alkoxy containing from 1 to 6, both inclusive, carbon atoms in the alkyl group, hydrogen or alkyl of from 1 to 6, both inclusive, carbon atoms; each R'''' independently represents hydrogen or alkyl of from 1 to 6, both inclusive, carbon atoms; each R'''''' independently represents hydrogen or alkyl of from 1 to 6, both inclusive, carbon atoms, or both R'''''' groups taken together represent oxo( O); X represents halo; and each n independently represents an integer of from 0 to 1, both inclusive. The terms ''''halo'''' and ''''halide'''' are employed herein to designate occurrences of bromine, chlorine, and iodine. The adamantane compounds of formulae VII and VIII are useful as agents to achieve a depressant action on the central nervous system of warm blooded animals. The adamantane compounds of Formulae I, II, III, IV, V and VI are useful as intermediates in the synthesis of the compounds of Formulae VII and VIII.
参考标题:A Metal‐free Direct Arene C−h Amination 作者:Tao Wang,Marvin Hoffmann,Andreas Dreuw,Edina Hasagić,Chao Hu,Philipp M. Stein,Sina Witzel,Hongwei Shi,Yangyang Yang,Matthias Rudolph,Fabian Stuck,Frank Rominger,Marion Kerscher,Peter Comba,A. Stephen K. Hashmi |发布日期:2021.6.8 摘要:The Synthesis Of Aryl Amines Via The Formation Of A C−n Bond Is An Essential Tool For The Preparation Of Functional Materials, Active Pharmaceutical Ingredients And Bioactive Products. Usually, This Chemical Connection Is Only Possible By Transition Metal-Catalyzed Reactions, Photochemistry Or Electrochemistry. Here, We Report A Metal-Free Arene C−h Amination Using Hydroxylamine Derivatives Under Benign
合成参考文献
摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 289. 摘要:Aitken, R. A., Science of Synthesis Knowledge Updates, (2018) 3, 304. 摘要:Kleoff, M.; Omoregbee, K.; Zimmer, R., Science of Synthesis Knowledge Updates, (2018) 4, 214.