- REACTIONS OF 2-TRIMETHYLSILYLYHIAZOLE WITH ACYL CHLORIDES AND ALDEHYDES SYNTHESIS OF NEW THIAZOL-2-YL DERIVATES
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2-Trimethylsilylthiazole (1) undergoes ipso-substitution of the silyl group with various acyl chlorides and ethyl chloroformate affording 2-acylthiazoles (2)-(5) but adds by the carbon-silicon bond to the carbonyl group of aldehydes yielding thiazol-2-yl-trimethylsiloxy-methane derivates (7).
- Medici, Alessandro,Fantin, Giancarlo,Fogagnolo, Marco,Dondini, Alessandro
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- Substituted pyrrole chromone compound or pharmaceutically acceptable salt thereof and preparation method and application thereof
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The invention discloses a substituted pyrrole chromone compound or pharmaceutically acceptable salt thereof and a preparation method and application thereof. The structure of the compound or the pharmaceutically acceptable salt thereof is shown in the for
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Paragraph 0081; 0108-0111
(2019/01/23)
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- PYRAZOLO[4,3-D]THIAZOLE DERIVATIVES, AND PREPARATION AND THERAPEUTIC APPLICATION THEREOF
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The disclosure relates to a compound of formula (I): in which: R1, R2, R3 and R4 are as described in the specification, to compositions containing them and to their therapeutic use, especially as anticancer agen
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Page/Page column 13
(2009/07/18)
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- THIAZOLE PYRAZOLOPYRIMIDINES AS CRF1 RECEPTOR ANTAGONISTS
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The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological dise
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Page/Page column 26
(2008/06/13)
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- 1-(Aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
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Certain 1-(aromatic- or heteroaromatic-substituted-3-(heteroaromatic substituted)-1,3-propanediones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
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- Synthesis of (Trimethylsilyl)thiazoles and Reactions with Carbonyl Compounds. Selectivity Aspects and Synthetic Utility
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Synthetic routes to all possible regioisomeric mono- and bis(trimethylsilyl)thiazoles as well as to the tris(trimethylsilyl) derivative via lithiation-silylation sequences of the thiazole ring followed by selective protodesilylation in some cases are described. (Trimethylsilyl)thiazoles serve as thiazolyl donor synthons upon reaction with carbonyl compounds (ketenes, acyl chlorides, aldehydes) for the preparation of mono- and bis-substituted thiazoles in very good yields.Carbodesilylation occurs more readily at the 2- than 5-position, whereas no reaction takes place at the 4-position.A mechanism via a thiazolium 2-ylide as an intermediate is suggested for the carbodesilylation at the 2-position.
- Dondoni, Alessandro,Fantin, Giancarlo,Fogagnolo, Marco,Medici, Alessandro,Pedrini, Paola
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p. 1748 - 1761
(2007/10/02)
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- NEW PERSPECTIVES IN THIAZOLE CHEMISTRY
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Carbon-carbon bond forming reactions at C-2 of the thiazole ring have been carried using two strategies, one involving the addition of organometallic reagents (lithium carbanions of esters, Grignard salts, silyl enol ethers, silyl ketene acetals, silylazoles) to N-acylthiazolium salts; the other involving the addition of carbon electrophiles (ketenes, acyl chlorides, anhydrides, aldehydes) to N-acylthiazolium ylides generated in situ.The reactions have been applied to 1,3-thiazole and 2-trimethylsilyl-1,3-thiazole, the latter being more reactive than the former toward electrophiles.This methodology constitutes a new entry to a variety of functionalized thiazoles and thiazolines which are potential building blocks for the synthesis of natural compounds and analogues of biologically active molecules (penems, arylpropionic acids).Some ring transformations of thiazoles induced by carbon-sulfur bond cleavage are also described.The fundamental role played by the sulfur atom of the thiazole ring in the observed reactions is pointed out and briefly discussed.
- Dondoni, Alessandro
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