- NUCLEOSIDE AND NUCLEOTIDE CONJUGATE COMPOUNDS AND USES THEREOF
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This disclosure provides nucleoside and nucleotide conjugate compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases,
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Paragraph 0175
(2021/10/11)
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- Nitrile Synthesis by Aerobic Oxidation of Primary Amines and in situ Generated Imines from Aldehydes and Ammonium Salt with Grubbs Catalyst
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Herein, a Grubbs-catalyzed route for the synthesis of nitriles via the aerobic oxidation of primary amines is reported. This reaction accommodates a variety of substrates, including simple primary amines, sterically hindered β,β-disubstituted amines, allylamine, benzylamines, and α-amino esters. Reaction compatibility with various functionalities is also noted, particularly with alkenes, alkynes, halogens, esters, silyl ethers, and free hydroxyl groups. The nitriles were also synthesized via the oxidation of imines generated from aldehydes and NH4OAc in situ. (Figure presented.).
- Utsumi, Tatsuki,Noda, Kenta,Kawauchi, Daichi,Ueda, Hirofumi,Tokuyama, Hidetoshi
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supporting information
p. 3583 - 3588
(2020/08/05)
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- GALNAC DERIVATIVES
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Modified oligonucleotides comprising a GalNAc moiety of the present disclosure along with methods of making and use, e.g., against HBV are disclosed.
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Paragraph 0118
(2019/04/11)
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- Sulfonium alkylation followed by 'click' chemistry for facile surface modification of proteins and tobacco mosaic virus
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Alkylsulfonium salts (ASS) have been shown to act as powerful alkylating agents. However, few studies have addressed the application of sulfonium salts to the modification of biomolecules such as nucleic acids and proteins. Since these large biomolecules play important roles in biological processes, a convenient and fast method for their modification is greatly needed. In this work, for the first time, we used a tandem method of sulfonium alkylation and click chemistry (CuAAC) for modification of biomolecules. Fluorescent labeling of proteins and tobacco mosaic virus were successfully performed after simple incubation of biomolecules with sulfonium salts followed by azido-containing compound at room temperature. This facile bioconjugation assay based on ASS-CuAAC reactions should be useful in protein chemistry and bionanoscience.
- Yi, Long,Shi, Jie,Gao, Shuang,Li, Shibo,Niu, Congwei,Xi, Zhen
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supporting information; experimental part
p. 759 - 762
(2009/05/07)
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- Synthesis and biological activity of dialkylphosphocholines
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A series of dialkylphosphocholines were prepared and evaluated for their biological activity. The antiprotozoal activity was determined against Acanthamoeba lugdunensis. Compound 15 exhibited excellent trophocidal activity. None of the tested dialkylphosphocholines exhibited better fungicidal activity against Candida albicans than miltefosine. The antineoplastic activity was determined against HeLa. The most cytotoxic was compound 10, which was more active against tumor cells as against normal cells.
- Lukac, Milos,Mrva, Martin,Fischer-Fodor, Eva,Lacko, Ivan,Bukovsky, Marian,Miklasova, Natalia,Ondriska, Frantisek,Devinsky, Ferdinand
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scheme or table
p. 6346 - 6349
(2010/06/11)
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- Phospholipid derivatives
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Phospholipid derivatives of the formula: STR1 wherein R1 is a higher alkyl, acylmethyl or alkylcarbamoyl group which may be substituted by cycloalkyl; R2 is a lower alkyl which may be substituted by carboxy, formyl or lower acyl, a carbamoyl or thiocarbamoyl group which is substituted by lower alkyl, or an acetoacetyl group; R3, R4 and R5 are independently hydrogen or lower alkyl, or STR2 represents a cyclic ammonio group; and n represents an integer of 8 to 14, and salts thereof have antitumor activity.
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- HIGH-YIELD CATALYTIC METATHESIS OF ALKENYL TOSYLATES WITH APPLICATIONS IN ORGANIC SYNTHESIS
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Alkenyl tosylates of the type RCH=CH(CH2)nOTs undergo metathesis using a WCl6-Me3SnCl catalyst system, producing difunctionalised alkenes of the type TsO(CH2)nCH=CH(CH2)nOTs (n=7,8, and 9); examples of the use of
- Daly, Daniel G.,McKervey, M. Anthony
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p. 2997 - 2998
(2007/10/02)
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