Abstract:
AIM AND OBJECTIVE:Thiazol-2-imine derivatives are interested for their pharmaceutical and biologic activities. A literature survey reveals that there have been no any reports on the synthesis of thiazol-2-imine derivatives without substituents in position C-4 and C-5 via one-pot reaction. Herein we report an efficient one-pot route for synthesis of these compounds in good to high yields. MATERIALS AND METHOD:To a stirred mixture of amine (1 mmol) and phenylisothiocyanate (1 mmol) in EtOH (2 ml), KI (0.1 mmol) and DABCO (0.2 mmol) were added under reflux condition. Then α- chloroacetaldehyde (2 mmol) was added drop wise to the reaction mixture. After completion of the reaction, the product was purified over a silica gel short column (EtOAc/n-Hexane, 1:9). RESULTS:One pot reaction of primary amine, phenylisocyanate, and α-chloroacetaldehyde was carried out in the presence of various base and KI in different solvents. It was found that the maximum yield was obtained when the temperature reaches to the boiling point of EtOH. Comparing the reaction results in EtOH, CH3CN, THF, CH2Cl2, and H2O at reflux in the presence of various base, demonstrate that the yield of reaction in EtOH in the presence of DABCO was the most effective. When the reaction runs at the 20 mol% of the DABCO and 10 mol% of the KI, the yield and the time of the reaction were excellent. CONCLUSION:One-pot procedure can be used for the synthesis of thiazol-2-imine derivatives via the reaction of primary amines, α-chloroacetaldehyde, and phenylisothiocyanate in the presence of a catalytic amount of DABCO and potassium iodide in ethanol.
journal_name
Comb Chem High Throughput Screenjournal_title
Combinatorial chemistry & high throughput screeningauthors
Nasiri F,Sabahi-Agabager Ldoi
10.2174/1568009617666161107093942subject
Has Abstractpub_date
2017-01-01 00:00:00pages
35-40issue
1eissn
1386-2073issn
1875-5402pii
CCHTS-EPUB-79535journal_volume
20pub_type
杂志文章abstract::Two approaches were utilized to increase the throughput of pulsed ultrafiltration assays of ligand binding to human serum albumin, reducing the volume of the ultrafiltration chamber and combining pulsed ultrafiltration with high performance liquid chromatography-atmospheric pressure chemical ionization mass spectromet...
journal_title:Combinatorial chemistry & high throughput screening
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journal_title:Combinatorial chemistry & high throughput screening
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journal_title:Combinatorial chemistry & high throughput screening
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abstract:AIM AND OBJECTIVE:Lysine acetylation, as one type of post-translational modifications (PTM), plays key roles in cellular regulations and can be involved in a variety of human diseases. However, it is often high-cost and time-consuming to use traditional experimental approaches to identify the lysine acetylation sites. ...
journal_title:Combinatorial chemistry & high throughput screening
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doi:10.2174/1386207320666170314093216
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journal_title:Combinatorial chemistry & high throughput screening
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abstract::Therapeutic options for many infections are extremely limited and at crisis point. We run the risk of entering a second pre-antibiotic era. There had been no miracle drug for the patients infected by resistant microbial pathogens. Most of the very few new drugs under development have problems with their toxicity, or p...
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journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
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journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章,评审
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journal_title:Combinatorial chemistry & high throughput screening
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journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:10.2174/1386207013330788
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journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
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abstract:AIM AND OBJECTIVE:Flap endonuclease-1 (FEN1) plays a central role in DNA replication and DNA damage repair process. In mammals, FEN1 functional sites variation is related to cancer and chronic inflammation, and supports the role of FEN1 as a tumor suppressor. However, FEN1 is overexpressed in multiple types of cancer c...
journal_title:Combinatorial chemistry & high throughput screening
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doi:10.2174/1386207322666190704095602
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journal_title:Combinatorial chemistry & high throughput screening
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journal_title:Combinatorial chemistry & high throughput screening
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journal_title:Combinatorial chemistry & high throughput screening
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journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:10.2174/1386207322666190419110724
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journal_title:Combinatorial chemistry & high throughput screening
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journal_title:Combinatorial chemistry & high throughput screening
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journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:10.2174/1386207323666200407080352
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journal_title:Combinatorial chemistry & high throughput screening
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doi:10.2174/1386207317666141024152910
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abstract::Recent studies have suggested that both constitutive androstane receptor (CAR) and pregnane X-receptor (PXR) are involved in the induction of rat liver microsomal cytochrome P-450 (CYP) 2B and 3A through a mechanism called cross-talk. In this study we intend to determine if a PXR-reporter gene assay could be used for ...
journal_title:Combinatorial chemistry & high throughput screening
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doi:10.2174/1386207054020822
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abstract:OBJECTIVE:The aim of this study areto screen MicroRNAs (miRNAs) related to the prognosis of lung adenocarcinoma (LUAD) and to explore the possible molecular mechanisms. METHODS:The data for a total of 535 patients with LUAD data were downloaded from The Cancer Genome Atlas (TCGA) database. The miRNAs for LUAD prognosi...
journal_title:Combinatorial chemistry & high throughput screening
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abstract::In the life cycle of hepatitis C virus (HCV), NS3/NS4A protease has been proved to play a vital role in the replication of the HCV virus. Narlaprevir and its derivatives, the inhibitors of NS3/NS4A, would be potentially developed as important anti-HCV drugs in the future. In this study, quantitative structure-activity...
journal_title:Combinatorial chemistry & high throughput screening
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更新日期:2012-07-01 00:00:00
abstract:AIM AND OBJECTIVE:In the last decades, cancer has become a major problem in public health all around the globe. Chimeric chemical structures have been established as an important trend on medicinal chemistry in the last years. Thiazacridines are hybrid molecules composed of a thiazolidine and acridine nucleus, both pha...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
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