31408-23-8

Upstream product

• 86139-82-4 methoxy-3 phenyl-2 propenal 
• 113-00-8 guanidine nitrate 
• 402960-38-7 5-(4,4,5,5-tetramethyl[1,3,2]dioxaborolan-2-yl)pyrimidin-2-ylamine 
• 29110-75-6 N'-tosyl phenylhydrazine 
• 7752-82-1 5-bromo-2-aminopyrimidine 
• 887757-48-4 2-(4-(difluoromethoxy)phenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane 
• 22536-62-5 2-chloro-5-phenypyrimidine 
• 98-80-6 phenylboronic acid 
• 1445-39-2 2-amino-5-iodopyrimidine 
• 5905-69-1 1-bromo-4-(difluoromethoxy)benzene 
• 591-50-4 iodobenzene 
• 936250-22-5 (2-aminopyrimidin-5-yl)boronic acid 
• 108-86-1 bromobenzene 
• 119072-55-8 tert-butylisonitrile 

Downstream Products

• 85658-61-3 2-chloro-5-phenylpyrimidine 1-oxide 
• 726138-32-5 2-(4-bromo-phenyl)-6-phenyl-imidazo[1,2-a]pyrimidine 
• 328232-76-4 trans-3-oxo-N-(5-phenylpyrimidin-2-yl)-3H-spiro[6-aza-2-benzofuran-1,1'-cyclohexane]-4'-carboxamide 
• 1380235-02-8 N-butyl-5-phenylpyrimidin-2-amine 
• 328232-44-6 Trans-3'oxo-N-(5-phenyl-2-pyrimidinyl)spiro[cyclohexane-1,1'(3'H)-isobenzofuran]-4-carboxamide 
• 1192312-63-2 trans-3-oxo-N-(5-phenylpyrimidin-2-yl)-3H-spiro[7-aza-2-benzofuran-1,1'-cyclohexane]-4'-carboxamide 
• 328232-63-9 trans-3-oxo-N-(5-phenylpyrimidin-2-yl)-3H-spiro[5-aza-2-benzofuran-1,1'-cyclohexane]-4'-carboxamide 
• 328232-54-8 trans-3-oxo-N-(5-phenylpyrimidin-2-yl)-3H-spiro[4-aza-2-benzofuran-1,1'-cyclohexane]-4'-carboxamide 
• 78533-68-3 2-amino-5-phenyl-1,4,5,6-tetrahydropyrimidine 

Relevant academic research and scientific papers

Palladium-catalyzed remote C-H functionalization of 2-aminopyrimidines

A straightforward strategy was developed for the arylation and olefination at the C5-position of the N-(alkyl)pyrimidin-2-amine core with readily available aryl halides and alkenes, respectively. This approach was highly regioselective, and the transformation was achieved based on two different (Pd(ii)/Pd(iv)) and (Pd(0)/Pd(ii)) catalytic cycles.

Asymmetric pyrene derivatives comprising amine group including heteroaryl group and organic light-emitting diode including the same

The present invention relates to a pyrene derivative represented by [chemical formula A] or [chemical formula B], and an organic light emitting diode comprising the same, wherein substituents Py_1, Py_2, Ar_1, Ar_2, Z, and m are defined in the detailed de

Probing the Scope of the Amidine–1,2,3-triazine Cycloaddition as a Prospective Click Ligation Method

Despite recent achievements in the development of chemical reactions enabling selective modification of complex biomolecules, the demand for fast and efficient methodologies that allow the attachment of various functional groups to these systems is the subject of intense research. Here, we report on the study of the amidine–1,2,3-triazine cycloaddition reaction, which has the potential to address many of the challenges associated with the development of such chemistry. We describe an optimized protocol leading to the in situ formation of free amidine bases, which directly react in the cycloaddition reaction with 1,2,3-triazines. Our kinetic studies reveal the structural features determining the reaction rates. Finally, we show that the amidine–1,2,3-triazine cycloaddition is extraordinarily selective and orthogonal to other popular ligation reactions. The pros and cons of the methodology are presented.

CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF

Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.

The Dimroth rearrangement as a probable cause for structural misassignments in imidazo[1,2-a]pyrimidines: A 15N-labelling study and an easy method for the determination of regiochemistry

Structural misassignments are often seen for complex natural products, but this can also be an issue with seemingly simpler structures. In this paper, we describe how, using a 15N-labelled analogue, we established that the Dimroth rearrangement

Aminoguanidine hydrazone derivatives as non-peptide NPFF1 receptor antagonists reverse opioid induced hyperalgesia

Neuropeptide FF receptors (NPFF1R and NPFF2R) and their endogenous ligand Neuropeptide FF have been shown previously to display anti-opioid properties and to play a critical role in the adverse effects associated with chronic administrations of opiates including the development of opioid-induced hyperalgesia and analgesic tolerance. In this work, we sought to identify novel NPFF receptors ligands by focusing our interest on a series of heterocycles as rigidified non-peptide NPFF receptor ligands, starting from already described aminoguanidine hydrazones (AGH's). Binding experiments and functional assays highlighted AGH 1n and its rigidified analog 2-amino-dihydropyrimidine 22e for in vivo experiments. As earlier shown with the prototypical dipeptide antagonist RF9, both 1n and 22e reduced significantly the long lasting fentanyl-induced hyperalgesia in rodents. Altogether these data indicate that AGH rigidification maintains nanomolar affinities for both NPFF receptors, while improving antagonist character towards NPFF1R.

Exemplifying Prediction of Preferred Coupling Partners in Developing a Buchwald-Hartwig Coupling for the Synthesis of a c-Kit Inhibitor

Two convergent syntheses for compound 1 are described that apply Buchwald-Hartwig coupling as the key step. This development work provides a direct comparison of the coupling results from different coupling partners and illustrates that more efficiency ca

2-polysubstituted aromatic ring-pyrimidine derivative and preparation and medical application

The invention provides a 2-polysubstituted aromatic ring-pyrimidine derivative, an optical isomer of the derivative or a medically acceptable salt or solvate of the derivative, and application of the compound, the optical isomer of the derivative or the medically acceptable salt or solvate of the derivative in preparing antineoplastic medicine. According to the 2-polysubstituted aromatic ring-pyrimidine derivative, by adopting N-substituted pyridine-2-minopyrimidine as a lead compound obtained based on virtual screening of a structure, a series of brand new small molecule Chk1 inhibitors are designed and synthesized, and a Chk1 kinase inhibitory activity test of a molecular level is conducted on the compound. Experiments prove that the compound is a Chk1 inhibitor with a strong antitumous effect, Chk1 kinase inhibitory activity and a prospect, and new cancer treating medicine, and can be used for treating solid tumor or leukemia related with human or animal cell proliferation. The 2-polysubstituted aromatic ring-pyrimidine derivative has a structure shown in the general formula I.

ANTIMITOTIC AMIDES FOR THE TREATMENT OF CANCER AND PROLIFERATIVE DISORDERS

Novel, antimitotic heteroaryl amides and pharmaceutically acceptable salts of Formula I where Ar, R5, R6, R8, R9, R11, X1, and X2 are as defined herein, as compounds for treatment and prevention of cancer and proliferative diseases and disorders.

WNT PATHWAY MODULATORS

The present invention relates to dihydropyrazolo[l,5-a]pyrimidine compounds of formula I, defined herein, as WNT pathways modulators, processes for making them, and pharmaceutical compositions comprising them. Methods of treatment of conditions mediated by WNT pathway signalling including cancer, fibrosis, stem cell and diabetic retinopathy, rheumatoid arthritis, psoriasis and myocardial infarction, comprising the compounds of formula I are also provided.