- A convenient conversion of α-aminoacids into NH-Boc protected α-aminoketones via imidazolides
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Imidazolides obtained from natural α-aminoacids react with a twofold excess of Grignard reagents to afford in satisfactory to good yields the corresponding NH-Boc protected α-aminoketones. Under optimized conditions the reaction with phenyl- and n-pentylm
- Bonini, Bianca F.,Comes-Franchini, Mauro,Fochi, Mariafrancesca,Mazzanti, Germana,Ricci, Alfredo,Varchi, Greta
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- REDOX DEHYDRATION COUPLING CATALYSTS AND METHODS RELATED THERETO
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This disclosure relates to synthetic coupling methods using catalytic molecules. In certain embodiments, the catalytic molecules comprise heterocyclic thiolamide, S-acylthiosalicylamide, disulfide, selenium containing heterocycle, diselenide compound, ditelluride compound or tellurium containing heterocycle. Catalytic molecules disclosed herein are useful as catalysts in the transformation of hydroxy group containing compounds to amides, esters, ketones, and other carbon to heteroatom or carbon to carbon transformations.
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- Synthesis of optically active N-protected α-aminoketones and α-amino alcohols
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A series of optically active N-protected α-aminoketones were synthesized via the Grignard reaction of the Weinreb amides of the N-tert-butoxycarbonyl amino acids. Reduction of the α-aminoketones by sodium borohydride resulted in the corresponding 1,2-amino alcohols.
- Zhou, Zheng Hong,Tang, Yi Long,Li, Kang Ying,Liu, Bing,Tang, Chu Chi
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p. 603 - 606
(2007/10/03)
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- NOVEL THIAZINE OR PYRAZINE DERIVATIVES
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An object of the present invention is to synthesize novel compounds having 3-oxo-3, 4-dihydro-2H-1, 4-thiazine or 2-oxo-1, 2, 3, 4-tetrahydropyrazine as a main skeleton. The present invention relates to compounds represented by the following general formula [I] and salts thereof. In the formula, X is S or R6-(A2)n-N, R1 and R2 are H, alkyl, cycloalkyl or aryl, R3 and R4 are H, alkyl, cycloalkyl, aryl or aromatic heterocycles, R5 is H, alkyl, cycloalkyl, aryl or -A3-A4-R7, R6 is H, alkyl, cycloalkyl, OH, alkoxy, aryl, aryloxy or an aromatic heterocycle, R7 is H, alkyl, OH, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle, A1 is alkylene, A2 is carbonyl or sulfonyl, A3 is alkylene, and A4 is carbonyl or oxalyl.
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- Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors
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A series of succinyl hydroxamate MMP inhibitors were prepared incorporating an aryl amino ketone moiety in place of the more typical C- terminal amino acid amides. Compounds of the C-terminal ketone series displayed potent inhibition of MMPs. Several comp
- Sheppard, George S.,Florjancic, Alan S.,Giesler, Jamie R.,Xu, Lianhong,Guo, Yan,Davidsen, Steven K.,Marcotte, Patrick A.,Elmore, Ildiko,Albert, Daniel H.,Magoc, Terrance J.,Bouska, Jennifer J.,Goodfellow, Carole L.,Morgan, Douglas W.,Summers, James B.
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p. 3251 - 3256
(2007/10/03)
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