564483-40-5

Upstream product

• 110-91-8 morpholine 
• 18437-66-6 N-(t-butoxycarbonyl)-4-chloroaniline 
• 2524-67-6 4-morpholino-4-yl-phenylamine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 60144-53-8 N-(tert-butoxycarbonyl)-4-fluoroaniline 

Downstream Products

• 652153-65-6 (4-chloro-[1,3,5]triazin-2-yl)-(4-morpholin-4-ylphenyl)carbamic acid tert-butyl ester 
• 903587-21-3 {6-[3-(2-chloro-6-methyl-phenyl)-1-methyl-ureido]-pyrimidin-4-yl}-(4-morpholin-4-yl-phenyl)-carbamic acid tert-butyl ester 
• 903587-20-2 {6-[3-(2,6-dichloro-phenyl)-1-methyl-ureido]-pyrimidin-4-yl}-(4-morpholin-4-yl-phenyl)-carbamic acid tert-butyl ester 
• 903587-22-4 {6-[3-(2-chloro-phenyl)-1-methyl-ureido]-pyrimidin-4-yl}-(4-morpholin-4-yl-phenyl)-carbamic acid tert-butyl ester 
• 903587-15-5 (6-methylamino-pyrimidin-4-yl)-(4-morpholin-4-yl-phenyl)-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Ru(II)-Catalyzed Amination of Aryl Fluorides via η6-Coordination

We developed a Ru/hemilabile-ligand-catalyzed nucleophilic aromatic substitution (SNAr) of aryl fluorides as the limiting reagents. Significant ligand enhancement was demonstrated by the engagement of both electron-rich and neutral arenes in the SNAr amination without using excess arenes. Preliminary mechanistic studies revealed that the nucleophilic substitution proceeds on a η6-complex of the Ru catalyst and the substrate, and the hemilabile ligand facilitates dissociation of products from the metal center.

Preparation method of Rivaroxaban intermediates

The invention discloses a preparation method of Rivaroxaban intermediates. The invention relates to a green and efficient preparation method of 4-(4-aminophenyl)morpholinyl-3-one and an amino protected derivative thereof. A structure of a formula II is obtained through an oxidation reaction of a structure of a formula II, and a structure of a formula I can be obtained through a deprotection reaction of the structure of the formula II, wherein the compound I and the compound II are both important intermediates for synthesizing the anticoagulation drug Rivaroxaban. Potassium permanganate is usedas an oxidizing agent in the oxidation reaction, tetraethyl benzyl ammonium chloride (TEBAC) is used as a phase transfer catalyst, dichloromethane is used as a solvent, and the reaction temperature in the oxidation reaction is 15-55 DEG C. The invention provides the preparation method of the Rivaroxaban intermediates, and the preparation method has the advantages that the raw materials are cheapand easily available, the reactions are mild in condition and are easy to operate, the preparation method is green and is friendly to the environment, the intermediate products and the final product are easy to purify, the total yield is high, industrial production is easy to realize, and the preparation method is effective and practical.

Development of N-4,6-pyrimidine-N-alkyl-N′-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase

A new class of lymphocyte specific tyrosine kinase (lck) inhibitors based on an N-4,6-pyrimidine-N-alkyl-N′-phenyl urea scaffold is described. Many of these compounds showed low-nanomolar inhibition of lck kinase activity as well as IL-2 synthesis from Ju

Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors

On the basis of previous studies, we identified pyrazine-pyridine A as a potent vascular endothelial growth factor inhibitor and pyrimidine-pyridine B as a moderately potent cyclin dependent kinase (CDK) inhibitor. A proposed combination of CGP-60474 and

SUBSTITUTED TRIAZINE KINASE INHIBITORS

The present invention provides substituted 1,3,5-triazine compounds as kinase inhibitors and a method for treating or ameliorating a kinase mediated disorder.

Expanding Pd-catalyzed C-N bond-forming processes: The first amidation of aryl sulfonates, aqueous amination, and complementarity with Cu-catalyzed reactions

The first general method for the Pd-catalyzed amination of aryl tosylates and benzenesulfonates was developed utilizing ligand 1, which belongs to a new generation of biaryl monophosphine ligands. In addition, the new catalyst system for the first time enables amidation of aryl arenesulfonates and aqueous amination protocols that do not necessitate the use of cosolvents. The substrate scope has been significantly expanded to include aryl halides containing primary amides and free carboxylic acid groups. In the case of multifunctional substrates, the Pd-catalyzed amination can provide selectivity that is complementary to the Cu-catalyzed C-N bond-forming processes. Copyright