35970-82-2

Upstream product

• 42518-42-3 2,4-dichloro-5,6-dimethylthieno<2,3-d>pyrimidine 
• 51486-04-5 2-amino-4,5-dimethylthiophene-3-carboxamide 
• 100-28-7 4-Nitrophenyl isocyanate 
• 103-71-9 phenyl isocyanate 
• 622-58-2 p-Tolylisocyanate 
• 614-68-6 2-tolyl isocyanate 
• 2909-38-8 m-chlorophenyl isocyanate 
• 109-90-0 ethyl isocyanate 
• 4651-93-8 2-amino-4,5-dimethylthiophene-3-carboxylic acid methyl ester 
• 57-13-6 urea 
• 4651-94-9 2-amino-4,5-dimethylthiophene-3-carbonitrile 
• 124-38-9 carbon dioxide 
• 4815-24-1 2-amino-4,5-dimethyl-3-thiophenecarboxylic acid ethyl ester 
• 312607-42-4 ethyl 4,5-dimethyl-2-ureidothiophene-3-carboxylate 

Downstream Products

• 42518-42-3 2,4-dichloro-5,6-dimethylthieno<2,3-d>pyrimidine 

Relevant academic research and scientific papers

THIENO PYRIMIDINES AS FERROPORTIN INHIBITORS

The subject matter described herein is directed to ferroportin inhibitor compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries.

Preparation method of heterocyclicpyrimidinedione compound

The invention discloses a preparation method of a heterocyclicpyrimidinedione compound and relates to the technology of medicinal chemistry. The preparation method comprises the following steps: 1) mixing an o-amino formonitrile heterocyclic compound and a catalyst to form a mixture, wherein the catalyst is [HDBN][TFE]; 2) in a CO2 environment, heating the mixture and reacting; 3) when the temperature is reduced to room temperature, adjusting the pH value to neutrality, and extracting, separating and collecting the an organic phase; drying, filtering and then vaporizing; performing column chromatography separation to obtain the heterocyclicpyrimidinedione compound. The preparation method disclosed by the invention has the advantages of low cost, environmental friendliness, simple preparation process and wide application range of substrate.

Ionic liquid promoted synthesis of heterocycle-fused pyrimidine-2,4(1H,3H)-diones utilising CO2

An efficient ionic liquid system was developed for the preparation of various heterocycle-fused pyrimidine-2, 4(1H,3H)-diones in moderate to excellent yields (52–95%). It was found that [HDBN+][TFE?], a simple and easily prepared ionic liquid, could act as both the solvent and reaction promoter, and that the reactions could be efficiently carried out at atmospheric pressures of CO2.

Design, Synthesis, and SAR Studies of Heteroarylpyrimidines and Heteroaryltriazines as CB2R Ligands

Herein we describe the design and synthesis of a new series of heteroarylpyrimidine/heteroaryltriazine derivatives on the basis of quinazoline-2,4(1H,3H)-diones as CB2R-selective ligands using a bioisosterism strategy. An acetamide group was explored to displace the enamine linker of the lead compound for the purpose of stereoisomerism elimination and hydrophilicity increase. As a result, some of the synthesized compounds showed high bioactivity and selectivity for CB2R in calcium mobilization assays, and four displayed CB2R agonist activity, with EC50 values below 30 nm. The compound exhibiting the highest agonist activity toward CB2R (EC50=7.53±3.15 nm) had a selectivity over CB1R of more than 1328-fold. Moreover, structure–activity relationship (SAR) studies indicated that the substituents on the nucleus play key roles in the functionality of a ligand, with one such example demonstrating CB2R antagonist activity. Additionally, molecular docking simulations were conducted with the aim of better understanding of these new derivatives in relation to the structural requirements for agonists/antagonists binding to CB2R.

Heteroarylpyrimindinedione derivative and use thereof

The invention provides a heteroarylpyrimindinedione derivative and use thereof. The heteroarylpyrimindinedione derivative comprises a compound with a structure shown as general formula I, and a pharmaceutically acceptable salt or hydrate thereof. The derivative is obtained by chemical synthesis, and pharmacological experiments prove that the active ligand with cannabinoid type II receptor CB2 can be used for preparation of drugs for prevention and mitigation of CB2 receptor-mediated diseases, and the drug is cannabinoid CB2 receptor agonist's agonist, partial agonist, inverse agonist or antagonist. And the general structural formula I is shown as the specification.

2,4-Diaminothienopyrimidines as orally active antimalarial agents

A novel series of 2,4-diaminothienopyrimidines with potential as antimalarials was identified from whole-cell high-throughput screening of a SoftFocus ion channel library. Synthesis and structure-activity relationship studies identified compounds with potent antiplasmodial activity and low in vitro cytotoxicity. Several of these analogues exhibited in vivo activity in the Plasmodium berghei mouse model when administered orally. However, inhibition of the hERG potassium channel was identified as a liability for this series.

Investigation into the reaction of 2-amino- 4,5-dimethylthiophene-3- carboxamide with iso(and Isothio)cyanates under microwave irradiation

The reaction of 2-amino-4,5-dimethyl-thiophene-3-carboxamide with iso(and isothio) cyanates for the synthesis ofthieno[2,3-d]pyrimidines has been investigated. The reactions under microwave irradiation in the presence of N,N-dimethyl acetamide as solvent

Thieno Compounds. Part 5: Basically Substituted Thienopyrimidines

Derivatives of Thienopyrimidine are the analogous structures of quinazolines, which are used in therapy, especially against hypertonia.Some new basically substituted thienopyrimidines were synthesized from 3,4-dihydro-4-oxothienopyrimidines with 4-chlorothienopyrimidines as intermediates.The corresponding 2,4-dibasic derivatives were received in the same way by transformation of the 1,2,3,4-tetrahydro-2,4-dioxothienopyrimidines.Derivatives with two different basic groups were obtained by a step-wise substitution of the both chlorine-atoms.I the case of a reaction with an aliphatic amine to substitute the chlorine in position 4 followed by a reaction with an aromatic amine both the chlorine in position 2 and the basic group in position 4 are replaced.