81066-94-6

Upstream product

• 14533-93-8 Methyl (E)-2-cyano-3-methoxy-3-phenylpropenoate 
• 113-00-8 guanidine nitrate 
• 593-85-1 diguanidine carbonate 
• 100-52-7 benzaldehyde 
• 105-56-6 ethyl 2-cyanoacetate 
• 105-34-0 methyl 2-cyanoacetate 
• 6041-23-2 methyl N-cyanobenzenecarboximidoate 
• 107-91-5 cyanoacetic acid amide 
• 50-01-1 guanidine hydrochloride 
• 716336-73-1 1-benzylideneurea 
• 124-46-9 guanidine hydrogen carbonate 
• 5873-90-5 methyl benzimidate hydrochloride 
• 6041-23-2 methyl N-cyanobenzenecarboximidoate 

Downstream Products

• 81066-97-9 2-amino-4-methoxy-6-phenyl-5-pyrimidinecarbonitrile 
• 5587-93-9 2,5,7-Triamino-4-phenylpyrimido<4,5-d>pyrimidine 
• 86700-28-9 2-Amino-4-phenyl-6-thioxo-1,6-dihydro-pyrimidine-5-carbonitrile 

Relevant academic research and scientific papers

Fullerene-C60/NH2: A recyclable heterogeneous catalyst for the green synthesis of chromene and pyrimidine derivatives and antibacterial evaluation

An effective procedure for the synthesis of amino-functionalized fullerene with diethylenetriamine (C60-NH2) is described. The obtained material was characterized by Fourier-transform infrared spectroscopy, X-ray diffraction, scanning electron microscopy, energy dispersive X-ray spectroscopy, elemental analysis, thermogravimetric measurements, and X-ray photoelectron spectroscopy. The catalytic activity of C60-NH2 was studied in multicomponent reactions for the synthesis of chromene and pyrimidine derivatives. The results revealed that C60-NH2 was very effective and the desired chromene and pyrimidine products were isolated in good to excellent yields 78%–97% and 81%–98%, respectively. Moreover, the C60-NH2 catalyst could be recycled and reused for at least eight runs without substantial loss in its activity, which makes our procedure environmentally benign. Antibacterial behavior of some of the synthesized products was studied against Gram-positive and Gram-negative bacteria using disk and well diffusion methods. The chromene 4g showed a good antibacterial activity against both bacterial strains Staphylococcus aureus and Serratia marcescens. A good antibacterial activity was also detected for chromene 4o and pyrimidine 7j against S. aureus. The chromene 4m, 4n and pyrimidine 7i compounds displayed a good activity against Micrococcus luteus as a Gram-positive bacterium.

With the promotion of the activity of SOD 1, 2, 3, 4 - tetrahydro pyrimidine compound green preparation method

The invention discloses a promoting activity of SOD 1, 2, 3, 4 - tetrahydro pyrimidine compound green preparation method, which belongs to the technical field of synthesis of the organic molecule of function. Technical proposal of the invention points are

Simple, multicomponent, ecofriendly, microwave-mediated route for the synthesis of antimicrobial 2-amino-6-aryl-4-(3 h)-pyrimidinones

In this work, we describe a multicomponent microwave-mediated synthesis of 10 2-amino-6-aryl-4-oxo-1,6-dihydro-pyrimidine-5-carbonitriles in good chemical yields (44-67%), four of them not related in earlier literature. All pyrimidinones synthesized herein had their antimicrobial activity evaluated against the following microorganisms: Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus. Two of the synthesized substances displayed good antimicrobial activity against P. aeruginosa and S. aureus, two bacteria responsible for nosocomial infections. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications for the following free supplemental resource(s): Full experimental and spectral details.]

HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase

The identification of novel, non-purine based inhibitors of xanthine oxidase is described. After a high-throughput screening campaign, an NMR based counterscreen was used to distinguish actives, which interact with XO in a reversible manner, from assay artefacts. This approach identified pyrimidone 1 as a reversible and competitive inhibitor with good lead-like properties. A hit to lead campaign gave compound 41, a nanomolar inhibitor of hXO with efficacy in the hyperuricemic rat model after oral dosing.

Amino-functionalized SBA-15 catalyzed one-step synthesis of 2-amino-5-cyano-4-hydroxy-6-aryl pyrimidines

A simple and efficient approach towards one-step synthesis of 2-amino-5-cyano-4-hydroxy-6-aryl pyrimidines has been developed. It is based on three-component condensation of aliphatic, aromatic or heterocyclic aldehydes, ethyl cyanoacetate and guanidinium carbonate in the presence of amino-functionalized SBA-15 catalyst in ethanol. In this chemical process, the tautomeric interconversion of pyrimidine derivatives has been observed. This efficient technique has the advantage to give 2-amino-pyrimidine derivatives using a heterogeneous catalyst in high yields, to be completed in short reaction times and to offer a simple product isolation procedure.

A novel and efficient one-pot synthesis of 2-aminopyrimidinones and their self-assembly

A three-component reaction of benzaldehyde derivatives, methyl cyanoacetate, and guanidinium carbonate affords 2-amino-4-aryl-1,6-dihydro-6- oxopyrimidine-5-carbonitriles and the four-component reaction of benzaldehyde derivatives, methyl cyanoacetate, and guanidinium hydrochloride in the presence of piperidine leads to piperidinium salts of pyrimidinones. X-ray crystallography data confirm self-assembly and H-bonding in these compounds.

Pyrimidine derivatives and their use for controlling undesired plant growth

Pyrimidine derivatives and their use for controlling undesired plant growth Compounds of the formula (I) and their use in the field of crop protection are described.

A novel and efficient one step synthesis of 2-amino-5-cyano-6-hydroxy-4-aryl pyrimidines and their anti-bacterial activity

The first simple and efficient approach towards one step synthesis of 2-amino-5-cyano-6-hydroxy-4-aryl pyrimidines has been developed by three component condensation of aromatic aldehydes, ethyl cyanoacetate and guanidine hydrochloride in alkaline ethanol

PYRIMIDOTHIOPHENE COMPOUNDS

Compounds of formula (1) are inhibitors of HSP90 activity in vitroor in vivo, and of use in the treatment of inter alia, cancer: wherein R2 is a group of formula -(Ar1)m-(Alk1)P-(Z)r-(Alk2)