- A Simple, Mild and General Oxidation of Alcohols to Aldehydes or Ketones by SO2F2/K2CO3 Using DMSO as Solvent and Oxidant
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A practical, general and mild oxidation of primary and secondary alcohols to carbonyl compounds proceeds in yields of up to 99% using SO2F2 as electrophile in DMSO as both the oxidant and the solvent at ambient temperature. No moisture- and oxygen-free conditions are required. Stoichiometric amount of inexpensive K2CO3, which generates easy to separate by-products, is used as the base. Thus, 5-gram scale runs proceeded in nearly quantitative yields by a simple filtration as the work-up. The use of a polar solvent such as DMSO, which usually promotes competing Pummerer rearrangement, is also noteworthy. This protocol is compatible with a variety of common N-, O-, and S-functional groups on (hetero)arene, alkene and alkyne substrates (68 examples). The protocol was applied (99% yield) to a formal synthesis of the important cholesterol-lowering drug Rosuvastatin. (Figure presented.).
- Zha, Gao-Feng,Fang, Wan-Yin,Leng, Jing,Qin, Hua-Li
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supporting information
p. 2262 - 2267
(2019/04/17)
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- A Transition-Metal-Free One-Pot Cascade Process for Transformation of Primary Alcohols (RCH2OH) to Nitriles (RCN) Mediated by SO2F2
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A new transition-metal-free one-pot cascade process for the direct conversion of alcohols to nitriles was developed without introducing an “additional carbon atom”. This protocol allows transformations of readily available, inexpensive, and abundant alcohols to highly valuable nitriles.
- Jiang, Ying,Sun, Bing,Fang, Wan-Yin,Qin, Hua-Li
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supporting information
p. 3190 - 3194
(2019/05/21)
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- A catalytic oxidation heterocyclic aromatic primary alcohol for the preparation of heterocyclic aromatic aldehyde
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The invention provides a method for preparing heterocyclic aromatic aldehyde by catalytically oxidizing heterocyclic aromatic primary alcohol. The method takes dioxovanadium nitrate as a catalyst and air as an oxidant; under a normal pressure condition, the heterocyclic aromatic primary alcohol is high-selectively oxidized into the heterocyclic aromatic aldehyde. The method provided by the invention has a high oxidization yield and a byproduct is water, so that the method is green, economical and environment-friendly; reaction conditions are moderate and the operation is simple. A catalysis system takes the air as the oxidant and non-metal metal as a catalyst, reaction conditions are moderate and the oxidization efficiency is high; the catalysis system is green and economical and can be used for efficiently catalyzing the heterocyclic aromatic primary alcohol into the corresponding heterocyclic aromatic aldehyde. Compared with a noble metal catalysis system and a catalysis system containing nitrogen-oxygen free radicals, the catalysis system has low oxidization reaction cost and has very high application value.
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Paragraph 0037; 0038
(2019/05/04)
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- BIOACTIVE COMPOUNDS FOR TREATMENT OF CANCER AND NEURODEGENERATIVE DISEASES
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The invention provides bioactive compounds for the treatment of various malconditions such as cancer and neurodegenerative diseases including Alzheimer's disease. The chemical compounds as disclosed herein are found to show bioactivity in bioassays related to these conditions. Pharmaceutical compositions, combinations and methods of synthesis are provided, as are methods of using the compound, compositions and combinations in the treatment of the diseases.
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Page/Page column 198
(2009/12/23)
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- AMINE COMPOUNDS AND USE THEREOF
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It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1):In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(=O) or NR11; and D is a group represented by the following general formula (4) or (6).-Q-Y-BIn the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7). z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26. In the above formulae, R1 to R26 each represents hydrogen, alkyl, alkenyl or alkynyl.
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Page/Page column 69
(2010/02/12)
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- Syntheses of 2-[(3,5-dimethyl-4-methoxypyridyl)alkyl]-benzothiazolidine derivatives as a potential gastric H+/K+-ATPase inhibitor
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A series of 2-[(3,5-dimethyl-4-methoxypyridyl)alkyl]benzothiazolidine derivatives were synthesized and tested their inhibitory effects on gastric H+/K+-ATPase. Compound 4d exhibited potent in vitro inhibitory activity.
- Yoon, Sung-Hwa,Seo, SeungKi,Lee, YoungHee,Hwang, SungKwan,Kim, Dong Yeon
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p. 1909 - 1912
(2007/10/03)
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