- OXADIAZOLONES AS TRANSIENT RECEPTOR POTENTIAL CHANNEL INHIBITORS
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The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
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Paragraph 0299-0302
(2018/06/12)
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- α-Alkylidene-γ-butyrolactone synthesis via one-pot C-H insertion/olefination: substrate scope and the total synthesis of (±)-cedarmycins A and B
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Abstract A system for the synthesis of α-alkylidene-γ-butyrolactones via a one-pot C-H insertion/olefination sequence is described. The process is based on the rhodium catalysed C-H insertion reaction of α-diazo-α-(diethoxyphosphoryl)acetates. The mild reaction conditions, operational simplicity and ready availability of starting materials are all key features. A wide range of successful reaction systems are reported (41 examples) highlighting the generality of the method. The application of this method in the total synthesis of the natural products (±)-cedarmycins A and B is also described.
- Lloyd, Matthew G.,D'Acunto, Mariantonietta,Taylor, Richard J.K.,Unsworth, William P.
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p. 7107 - 7123
(2015/02/19)
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- One-Carbon Homologation of Primary Alcohols and the Reductive Homologation of Aldehydes Involving a Jocic-Type Reaction
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(Trichloromethyl)carbinols, which are formed in one operation from either alcohols or aldehydes, can be converted into primary alcohols in a Jocic-type reaction involving LiBH4. The net result is a convenient two-step, one-carbon homologation of primary alcohols or a reductive one-carbon homologation of aldehydes featuring a broad substrate scope. The method is step-economical, and it nicely complements established one-carbon homologation strategies. (Trichloromethyl)carbinols, which are formed in one operation from either alcohols or aldehydes, can be converted into primary alcohols in a Jocic-type reaction involving LiBH4. The net result is a convenient two-step, one-carbon homologation of primary alcohols or a reductive one-carbon homologation of aldehydes featuring a broad substrate scope.
- Li, Zhexi,Gupta, Manoj K.,Snowden, Timothy S.
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p. 7009 - 7019
(2015/11/16)
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- Structure-activity relationships of the antimalarial agent artemisinin. 8. Design, synthesis, and CoMFA studies toward the development of artemisinin-based drugs against leishmaniasis and malaria
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Artemisinin (1) and its analogues have been well studied for their antimalarial activity. Here we present the antimalarial activity of some novel C-9-modified artemisinin analogues synthesized using artemisitene as the key intermediate. Further, antileish
- Avery, Mitchell A.,Muraleedharan, Kannoth M.,Desai, Prashant V.,Bandyopadhyaya, Achintya K.,Furtado, Marise M.,Tekwani, Babu L.
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p. 4244 - 4258
(2007/10/03)
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- ARTEMISININ-BASED PEROXIDE COMPOUNDS AS BROAD SPECTRUM ANTI-INFECTIVE AGENTS
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Described herein is the synthesis, bioassay results and utility of new C-9 and C-10 substituted artemisinin derivatives with easily functionalizable groups attached to the artemisinin skeleton through carbon chain or heteroatoms. Described also is the demonstration of this class of compounds for their broad-spectrum anti-parasitic activity. Certain of these analogs possess noticeable cytotoxicity deliberately focused on treatment of cancerous diseases.
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Page/Page column 22-23; 56
(2010/02/07)
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- The scope of catalytic asymmetric hydroboration/oxidation with rhodium complexes of 1,1'-(2-diarylphosphino-1-naphthyl)isoquinolines
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Preformed cationic Rh complexes of the title ligands are effective for the asymmetric hydroboration/oxidation of vinylarenes at ambient temperature. These vinylarenes may carry E- or Z-β substituents but not a substituents. Enantiomer excesses of up to 97% can be obtained in the most favourable cases. The enantioselectivity is moderately sensitive to the structure of the ligand: the difurylphosphino ligand gave superior results for electron-poor styrenes and the diphenylphosphino ligand the best results for electron-rich reactants. Mechanistic aspects are discussed.
- Doucet, Henri,Fernandez, Elena,Layzell, Timothy P.,Brown, John M.
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p. 1320 - 1330
(2007/10/03)
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- Preparation of N,N-dialkyl p-vinyl anilines
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A process of forming a dye mordant precursor for a photographic system by reacting a p-amino phenethyl alcohol with a trialkyl phosphate at a controlled temperature, and dehydrating the resultant p-dialkyl amino phenethyl alcohol with a strong alkali in the presence of a polymerization inhibitor.
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