461702-59-0

Upstream product

• 1722-12-9 2-chloropyrimidine 
• 106-40-1 4-bromo-aniline 
• 144-55-8 sodium hydrogencarbonate 
• 57356-49-7 phenyl-pyrimidin-2-yl-amine 
• 62-53-3 aniline 

Downstream Products

• 894400-67-0 N-(4-bromophenyl)-N-((pyridin-3-yl)methyl)pyrimidin-2-amine 
• 894400-59-0 N-(4-bromophenyl)-N-(4-methoxybenzyl)pyrimidin-2-amine 
• 894400-94-3 N-(4-bromophenyl)-N-phenylpyrimidin-2-amine 
• 894400-63-6 N-(4-bromophenyl)-N-butylpyrimidin-2-amine 
• 894400-71-6 N-(4-bromophenyl)-N-((thiazol-4-yl)methyl)pyrimidin-2-amine 
• 875-51-4 4-Bromo-2-nitroaniline 

Relevant academic research and scientific papers

Predictable site-selective functionalization: Promoter group assistedpara-halogenation ofN-substituted(hetero)aromatics under metal-free condition

Herein, regioselectivepara-C-H halogenation ofN-pyrimidyl (hetero)aromatics through SEAr (electrophilic aromatic substitution) type reaction is disclosed. SEAr type reaction has been utilized for the C5-bromination of indolines (para-selective) withN-bromosuccinimide under metal and additive-free conditions in good to excellent yields. The developed methodology is also applicable for iodination and challenging chlorination. The pyrimidyl group is identified as a reactivity tuner that also controls the regioselectivity. The present method is also applicable for selective halogenation of aniline, pyridine, indole, oxindole, pyrazole, tetrahydroquinoline, isoquinoline, and carbazole. DFT studies such as Fukui nucleophilicity and natural charge maps also support the observedp-selectivity. Post-functionalization of the title compound into the corresponding arylated, olefinated, and dihalogenated products is achieved in a one-pot, two-step fashion. Late-stage C-H bromination was also executed on drug/natural molecules (harmine, etoricoxib, clonidine, and chlorzoxazone) to demonstrate the applicability of the developed protocol.

Cp*IrIII-Catalyzed [3+2] Annulations of N-Aryl-2-aminopyrimidines with Sulfoxonium Ylides to Access 2-Alkyl Indoles Through C–H Bond Activation

The iridium-catalyzed aromatic C–H alkylation followed by intramolecular annulation reactions between N-aryl-2-aminopyridines and sulfoxonium ylides for the synthesis of 2-alkyl indoles is described. This highly efficient and step-economical cyclization r

Multiple Roles of the Pyrimidyl Group in the Rhodium-Catalyzed Regioselective Synthesis and Functionalization of Indole-3-carboxylic Acid Esters

A regioselective synthesis of indole-3-carboxylic acid esters from anilines and diazo compounds has been realized by making use of the pyrimidyl group-assisted rhodium-catalyzed C-H activation and C-N bond formation. The reaction proceeds under mild conditions, exhibits good functional group tolerance and scalability. Reutilization of the pyrimidyl directing group in the resulting products provided an efficient strategy for further C-7 functionalization of indoles. Moreover, the pyrimidyl moiety could be readily removed as a leaving group to offer various free N-H indoles.

N-(jodoethane phenylpropionic) Pirimidinyl production of amine derivative

PROBLEM TO BE SOLVED: To suppress generation of byproducts so as to improve production efficiency and purification efficiency of an N-(iodophenyl)pyrimidinylamine derivative, when producing the N-(iodophenyl)pyrimidinylamine derivative. SOLUTION: Th

Hypervalent iodine(III) promoted direct synthesis of imidazo[1,2-a] pyrimidines

An efficient and mild synthesis of imidazo[1,2-a]pyrimidine derivatives has been developed from readily available pyrimidyl arylamines or enamines through a hypervalent iodine-promoted intramolecular C-H bond cycloamination reaction. This protocol allows for the facile construction of biologically active bicyclic imidazo[1,2-a]pyrimidine skeletons as well as other imidazo[1,2-a]-type fused heterocycles.

Zinc base assisted amination of 2-chloropyrimidines by aniline derivatives at room temperature

The amination of 2-chloropyrimidines was performed with several aniline derivatives in the presence of tolylzinc bromide as a base. The organozinc compound has a profound effect on the reactivity of the amines, so that the reaction takes place at room tem

THERAPEUTIC OR PROPHYLACTIC AGENT FOR LEUKEMIA

A therapeutic or prophylactic agent for leukemia is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for leukemia according to the present invention shows the excellent absorbability and in vivo stability when orally administered, and exhibits prominent therapeutic or prophylactic effects.

THERAPEUTIC OR PROPHYLACTIC AGENT FOR ALLERGIC DERMATITIS

A therapeutic or prophylactic agent for allergic dermatitis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for allergic dermatitis according to the present invention has high therapeutic or prophylactic effect.

THERAPEUTIC OR PROPHYLACTIC AGENT FOR MULTIPLE SCLEROSIS

A therapeutic or prophylactic agent for multiple sclerosis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for multiple sclerosis according to the present invention shows the excellent absorbability and in vivo stability when orally administered, and exhibits high therapeutic or prophylactic effects.

GLYCINE DERIVATIVE AND USE THEREOF

The compounds in the present invention, for example, the compound represented by the formula: has an excellent therapeutic and prophylactic effects against inflammatory bowel disease. Further, they are excellent in absorption and in vivo stability when administered orally in comparison with conventional compounds. That is, the compounds can be administered orally, and can have excellent therapeutic or prophylactic effect sustained for a longer period of time.