- Generating Stereodiversity: Diastereoselective Fluorination and Highly Diastereoselective Epimerization of α-Amino Acid Building Blocks
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Diastereoselective fluorination of N-Boc (R)- and (S)-2,2-dimethyl-4-((arylsulfonyl)methyl)oxazolidines and a previously unknown diastereoselective epimerization at the fluorine-bearing carbon atom α to the sulfone was realized. Diastereoselectivities of both reactions were excellent for benzothiazolyl sulfones, allowing access to two enantiomerically pure diastereomers from one chiral precursor. To demonstrate synthetic utility, the benzothiazolyl sulfones were converted to diastereomerically pure (S,S)- and (R,S)-benzyl sulfones via sulfinate salts and to amino acids. To understand the diastereoselectivities, DFT analysis was performed.
- Wei, Wei,Khangarot, Rama Kanwar,Stahl, Lothar,Veresmortean, Cristina,Pradhan, Padmanava,Yang, Lijia,Zajc, Barbara
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p. 3574 - 3578
(2018/06/26)
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- Efficient synthesis of fused 1,2,3-triazolo-δ-lactams using Huisgen [3 + 2] dipolar cycloaddition "click-chemistry" in water
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A general approach for the quick synthesis of various 1,2,3-triazolo- δ-lactams has been described, which involves the Huisgen [3 + 2] dipolar cycloaddition of azides derived from different amino acids with dimethyl acetylenedicarboxylate in water followe
- Kumar, Indresh,Rode, Chandrashekhar V.
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p. 592 - 593
(2008/02/07)
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- Design, synthesis and activity as acid ceramidase inhibitors of 2-oxooctanoyl and N-oleoylethanolamine analogues
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The synthesis of novel N-acylethanolamines and their use as inhibitors of the aCDase is reported here. The compounds are either 2-oxooctanamides or oleamides of sphingosine analogs featuring a 3-hydroxy-4,5-hexadecenyl tail replaced by ether or thioether
- Grijalvo, Santiago,Bedia, Carmen,Triola, Gemma,Casas, Josefina,Llebaria, Amadeu,Teixido, Jordi,Rabal, Obdulia,Levade, Thierry,Delgado, Antonio,Fabrias, Gemma
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- ACRYLAMIDE DERIVATIVES AS VLA-1 INTEGRIN ANTAGONISTS AND USES THEREOF
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Compounds that are VLA-1 integrin antagonists are disclosed. Also disclosed are compositions containing such compounds, and methods of using such compounds in treating diseases mediated, at least in part, by the VLA-1 integrin.
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Page/Page column 304-305
(2010/02/10)
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- Synthesis of 2-amino-octa-4,7-dien-1-ol (2): Key intermediate for mycothiazole natural product and analogs
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Starting from L-aminoacids, facile methods for the preparation 2-aminocta-4,7-dien-ol with different stereochemistry have been developed as key intermediates of mycothiazole and analogs. Copyright Taylor & Francis, Inc.
- Mahler, Graciela,Serra, Gloria,Manta, Eduardo
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p. 1481 - 1492
(2007/10/03)
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- BISPHENYL COMPOUNDS USEFUL AS VITAMIN D3 RECEPTOR AGONISTS
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The present invention discloses bisphenyl compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, X, Y, W are defined herein after. These compounds are useful as pharmaceuticals.
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Page/Page column 322
(2010/02/14)
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- Design and optimization of new phosphine oxazoline ligands via high- throughput catalyst screening
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This paper uses the phosphine oxazoline ligands 1 and an allylation transformation (reaction 1) to illustrate the value of divergent ligand syntheses and high-throughput screening in catalyst discovery and optimization. Thus, a diverse set of ligands 1 (T
- Porte, Alexander M.,Reibenspies, Joe,Burgess, Kevin
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p. 9180 - 9187
(2007/10/03)
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- Guanidine derivatives compositions and use
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Compounds of the formula STR1 wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.
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