- I2-Promoted [3+2] Cyclization of 1,3-Diketones with Potassium Thiocyanate: a Route to Thiazol-2(3H)-One Derivatives
-
An I2-promoted strategy has been developed for the synthesis of thiazol-2(3H)-one derivatives from 1,3-diketones with potassium thiocyanate. This [3+2] cyclization reaction involves C?S and C?N bond formation and exhibits good functional group tolerance. A series of thiazol-2(3H)-one derivatives are obtained in moderate to good yields. (Figure presented.).
- An, Zhenyu,Liu, Yafeng,Yan, Rulong,Zhao, Pengbo
-
supporting information
p. 3240 - 3244
(2021/06/16)
-
- Direct route to 1,3-diketones by palladium-catalyzed carbonylative coupling of aryl halides with acetylacetone
-
Man up your magnesium! By employing a MgCl2/Et3N system, aryl diketones can be generated from the Pd-catalyzed carbonylative α-arylation of acetylacetone with aryl bromides (see scheme). The method is ideal for the introduction of carbon isotopes into more complex structures, since only stoichiometric amounts of carbon monoxide are employed. Copyright
- Korsager, Signe,Nielsen, Dennis U.,Taaning, Rolf H.,Lindhardt, Anders T.,Skrydstrup, Troels
-
supporting information
p. 17687 - 17691
(2014/01/17)
-
- Triketoacid inhibitors of HIV-integrase: A new chemotype useful for probing the integrase pharmacophore
-
Integrase is one of three enzymes expressed by HIV and represents a validated target for therapy. This study reports on the discovery of a new triketoacid-based chemotype that selectively inhibits the strand transfer reaction of HIV-integrase. SAR studies showed that the template binds to integrase in a manner similar to the diketoacid-based inhibitors. Moreover, comparison of the new chemotype to two different diketoacid templates led us to propose two aryl-binding domains in the inhibitor binding site. This information was used to design a new diketoacid template with improved activity against the enzyme.
- Walker, Michael A.,Johnson, Timothy,Ma, Zhuping,Banville, Jacques,Remillard, Roger,Kim, Oak,Zhang, Yunhui,Staab, Andrew,Wong, Henry,Torri, Albert,Samanta, Himadri,Lin, Zeyu,Deminie, Carol,Terry, Brian,Krystal, Mark,Meanwell, Nicholas
-
p. 2920 - 2924
(2007/10/03)
-
- Evaluation of TCS/ZnCl2 with acetic anhydride as an acetylating reagent for methylene ketones
-
A new route for the preparation of β-diketones which have applications in organic synthesis by the reaction of methylene ketones, acetic anhydride, TCS and ZnCl2 in the solvent methylene chloride at room temperature produces the corresponding β-diketones in excellent yield. Copyright Taylor & Francis Inc.
- Elmorsy, Saad S.,Badawy, Doria S.,Khatab, Tamer K.
-
p. 109 - 116
(2007/10/03)
-
- Ion pair first and second acidities of some β-diketones and aggregation of their lithium and cesium enediolates in THF
-
Ion pair pK values were measured for three β-diketones in THF, 1-3, with lithium and cesium counterions. The results showed variations with concentration indicative of aggregation of the metal enolates to dimers. Similarly, ion pair pK values could be det
- Facchetti, Antonio,Streitwieser, Andrew
-
p. 8345 - 8355
(2007/10/03)
-
- PHENYLPROPANOIDS AND OTHER DERIVATIVES FROM THAPSIA VILLOSA
-
Key Word Index - Thapsia villosa; Umbelliferae; roots; phenylpropanoids; hemanticine; guaianolides; thapsivillosin K. - Five phenylpropanoids related to hemanticine have been obtained from Thapsia villosa roots.We propose for these substances the trivial names isohelmanticine, neohelmanticine, isoneohelmanticine, epoxyhelmanticine and epoxyhelmanticine angelate.All these substances are based on (1S,2R)1-(3-methoxy-4,5-methylenedioxyphenyl)-1,2-propanediol, which is esterified variously by acetic, angelic, epoxyangelic and/or (2R,3S)2,3-dihydroxy-2-methylbutyric acids.We also report three C6-guaianolides and their hydrolysis products.The name thapsivillosin K is proposed for a new guaianolide.
- Teresa, J. De Pascual,Moran, Joaquin R.,Hernandez, Jose M.,Grande, M.
-
p. 2071 - 2074
(2007/10/02)
-