- Chemoenzymatic Dynamic Kinetic Resolution of Amines in Fully Continuous-Flow Mode
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In this study, lipase-mediated dynamic kinetic resolution (DKR) of various benzylic amines (1a-g) is presented which is realized in a so far unprecedented fully continuous-flow system. The DKR process applying sol-gel immobilized lipase B from Candida antarctica as biocatalyst, palladium on 3-aminopropyl-functionalized silica as racemization catalyst, isopropyl 2-ethoxyacetate as acylating agent, ammonium formate as hydrogen and nitrogen sources, and 2-methyl-2-butanol as solvent under regulated pressure provided the desired products in moderate to good yields with excellent enantiomeric excesses.
- Farkas, Emese,Oláh, Márk,F?ldi, Attila,Kóti, János,éles, János,Nagy, József,Gal, Cristian Andrei,Paizs, Csaba,Hornyánszky, Gábor,Poppe, László
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supporting information
p. 8052 - 8056
(2019/01/14)
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- 6-HYDROXY-4-OXO-1,4-DIHYDROPYRIMIDINE-5-CARBOXAMIDES AS APJ AGONISTS
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The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
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Paragraph 0878; 0879
(2017/10/10)
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- APELIN RECEPTOR AGONISTS AND METHODS OF USE
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The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
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Page/Page column 76; 77
(2017/12/28)
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- CYCLOAMINO DERIVATIVES AS GPR119 ANTAGONISTS
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Therapeutic compounds are disclosed having the general formula (I) that are useful for the treatment of metabolic disorders, including type II diabetes. The compounds have activity as agonists of GPR119. Compounds having the stereochemistry of formula (la) may also demonstrate DPP-IV inhibitory activity.
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Page/Page column 105
(2011/12/14)
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- Reaction of Carbenes with Cyclic Ethers in the Presence of Nucleophiles. A Three-Component Coupling Reaction
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Ternary reaction systems consisting of a carbene , a cyclic ether (THF, THP) and a protic nucleophile (alcohol, water, carboxylic acid, thiol, or amine) give the corresponding three-component coupling products which are produced via ethereal oxonium ylide intermediates.The mechanism leading to the product formation has been studied in which protonation of carbenes is excluded.
- Oku, Akira,Kimura, Kenji,Ohwaki, Shigeyoshi
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p. 391 - 397
(2007/10/02)
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