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1.
Abstract  A short and efficient sequence for the synthesis of a series of 4-(2-amino-5-thiazolyl)-pyrimidine-2-amines was developed. 1-Phenyl-2-(6-pyrimidinyl)-ethanones, obtained via Weinreb’s methodology, were used in a Hantzsch thiazole cyclization reaction, followed by introduction of the aniline moieties via nucleophilic substitution. Graphical abstract     相似文献   

2.
Abstract  In contrast to the results presented in a previous report, the direct conversion of alcohols to alkyl fluorides with triphenylphosphine and potassium fluoride in CCl4/DMF under mild conditions failed. Graphical Abstract     相似文献   

3.
Abstract  A simple, highly efficient, and green protocol has been developed for preparation of sulfides from alkyl or aryl thiols and benzyl-, allyl-, t-butyl, and adamantyl halides under solvent- and catalyst-free conditions. Graphical abstract     相似文献   

4.
Abstract  A Mild and efficient method for preparing amides by reaction of nitriles with benzhydrol and tertiary alcohols is described using polyvinylpolypyrrolidone-supported boron trifluoride. Selective amidation of benzhydrol in the presence of primary benzyl alcohols was also achieved. Graphical abstract     相似文献   

5.
Abstract  A very simple, convenient, and efficient procedure is reported for the 1,3-allylic carbonyl transposition of chalcones. The transposition can be achieved by reduction of chalcones to 1,3-diarylpropan-1-ols and dehydration of the latter to give 1,3-diarylpropenes followed by benzylic/allylic oxidation. Graphical abstract     相似文献   

6.
Abstract  4-Fluorobenzaldehyde was used for the preparation of 2-(4-fluorophenyl)thiazolidin-4-one derivatives which were allowed to react with chloroacetonitrile and acrylonitrile to produce 3-(2-(4-fluorophenyl)-4-oxothiazolidine3-yl)acetonitrile and 3-(2-(4-fluorophenyl)-4-oxothiazoledine-3-yl)propanenitrile. Biological evaluation of some of the compounds showed that many had promising antioxidant activity. Graphical Abstract     相似文献   

7.
Abstract  A series of peptide derivatives conjugated with N1-protected tryptophan residue was synthesized. The prepared compounds were tested for antimicrobial activity against four different bacterial species displaying different degrees of antibacterial activities or inhibitory actions. Graphical Abstract     相似文献   

8.
Abstract  New C-furyl glycosides bearing pyrazolines, isoxazolines, and dihydropyrimidine-2(1H)-thiones were synthesized in order to increase the number of tested compounds screened for antimicrobial activity. The antimicrobial activity screening showed that the pyrazoline derivatives were the most active compounds. Graphical abstract     相似文献   

9.
Abstract  Saccharin sulfonic acid was easily prepared by the reaction of saccharin with neat chlorosulfonic acid at room temperature. This reagent is efficiently able to catalyze the chemoselective trimethylsilylation of alcohols with hexamethyldisilazane in the presence of amines and thiols. Graphical abstract     相似文献   

10.
Abstract  A novel method for oxazine ring formation is established using the reaction of ammonium thiocyanate and acid chlorides with napthols in the presence of N-methylimidazole to afford [1,3]oxazine-4-thione derivatives in excellent yields. Graphical abstract     相似文献   

11.
Abstract  Potassium hydrazinecarbodithioate were prepared by treatment of acid hydrazides with carbon disulfide in the presence of potassium hydroxide. Reaction of this potassium salt with hydrazine hydrate, phenacyl bromide, or hydrazonoyl chlorides afforded 1,2,4-triazole, 1,3-thiazole, and 1,3,4-thiadiazoles. Reaction of 1,2,4-triazole with phenacyl bromide or hydrazonoyl chlorides afforded the corresponding 1,2,4-triazolo[3,4-b][1, 3, 4]-thiadiazines. All these new compounds were screened for antibacterial and antifungal activity. Some had promising activity. Graphical abstract     相似文献   

12.
Abstract  Synthesis of chelates from selected l-amino acids and triethylborane, and the mass spectra of the chelates, are described. Conditions for forming dimers between the chelates and the sodium ion are discussed, and structures are proposed for the dimers. Graphical abstract     相似文献   

13.
Abstract  A polymer-supported Lewis acid catalyst was prepared and found to be extremely efficient for the preparation of imidazole derivatives via three-component condensation of benzil, aldehydes, and ammonium acetate under mild conditions. The catalyst is stable and can be easily recovered and reused at least four times without any loss of activity. Graphical Abstract     相似文献   

14.
Abstract  Aromatic aldoximes were converted to the corresponding nitriles in good to excellent yields by employing phosphoric acid diethyl ester 2-phenylbenzimidazol-1-yl ester as reagent. The method was equally effective for oximes bearing electron-donating and electron-withdrawing substituents. Graphical Abstract     相似文献   

15.
Abstract  The enzymatic cyclization of phenoxyacetylcyanomethylenetriphenylphosphorane derivatives using pre-treated baker’s yeast cells, a rapid one-pot assembly of heteromacrocyclic compounds, is described. Graphical abstract     相似文献   

16.
Abstract  Catalytic transfer hydrogenation of α-tosyloxyarylketones mediated by a chiral rhodium complex using an azeotropic mixture of formic acid/triethylamine afforded the corresponding 1-arylethanediol monotosylates in excellent yield with high enantioselectivity. Graphical abstract     相似文献   

17.
Abstract  1-Ethyl-3-methylimidazolium bromide was used as a green recyclable alternative to volatile organic solvents for KOH catalyzed three-component synthesis of diethyl alkylsulfanylmethylmalonates from aldehydes, diethyl malonate, and alkylthiols. Graphical Abstract  A synthesis of diethyl alkylsulfanylmethylmalonates catalyzed by KOH in an ionic liquid   相似文献   

18.
Abstract  One-pot, three-components synthesis of 2,4,6-triarylpyridines and 5-unsubstituted-3,4-dihydropyrimidin-2(1H)-ones was performed under solvent-free conditions using molecular iodine as the catalyst in moderate to good product yields. Graphical abstract     相似文献   

19.
Abstract  A simple one-pot synthesis of functionalized ethyl 1,3-thiazole-5-carboxylates from the reaction of 2-chloro-1,3-dicarbonyl compounds with thioureas or thioamides in the presence of 1-butyl-3-methylimidazolium trifluoromethanesulfonate is described. Graphical abstract     相似文献   

20.
Abstract  An efficient one-pot reaction of dialkyl acetylenedicarboxylates with 2,4-dihydroxybenzo(or aceto)phenones in the presence of triphenylphosphine produces 5-hydroxy- and 7-hydroxycoumarin derivatives. The novel procedure features short reaction time, fairly good yields, and simple workup. Graphical abstract     相似文献   

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