17847-35-7

Upstream product

• 100-14-1 4-nitrobenzyl chloride 
• 75-04-7 ethylamine 
• 25105-58-2 N-(p-nitrobenzylidene)ethylamine 
• 50445-50-6 N-ethyl-4-nitrobenzamide 
• 555-16-8 4-nitrobenzaldehdye 
• 557-66-4 ethanamine hydrochloride 
• 100-11-8 1-bromomethyl-4-nitro-benzene 
• 34597-04-1 N-ethyl-N-acetylbenzylamine 
• 14321-27-8 N-ethylbenzylamine 

Downstream Products

• 247085-22-9 (4-aminobenzyl)-N-ethylcarbamic acid tert-butyl ester 
• 55245-74-4 C₁₀H₁₁ClN₂O₃ 

Relevant academic research and scientific papers

Zirconium-hydride-catalyzed site-selective hydroboration of amides for the synthesis of amines: Mechanism, scope, and application

Developing mild and efficient catalytic methods for the selective synthesis of amines is a longstanding research objective. In this respect, catalytic deoxygenative amide reduction has proven to be promising but challenging, as this approach necessitates selective C–O bond cleavage. Herein, we report the selective hydroboration of primary, secondary, and tertiary amides at room temperature catalyzed by an earth-abundant-metal catalyst, Zr-H, for accessing diverse amines. Various readily reducible functional groups, such as esters, alkynes, and alkenes, were well tolerated. Furthermore, the methodology was extended to the synthesis of bio- and drug-derived amines. Detailed mechanistic studies revealed a reaction pathway entailing aldehyde and amido complex formation via an unusual C–N bond cleavage-reformation process, followed by C–O bond cleavage.

COMPOUNDS FOR THE MODULATION OF CYCLOPHILINS FUNCTION

The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof useful as inhibitors of Cyclophilins and modulators of cyclophilin-like proteins. The invention also relates to uses of said compounds in the treatment of various disorders. Formula (I), wherein: R1 and R2 are each independently is selected from the group consisting of -R, -haloalkyl, -hydroxyalkyl, -OR, -C(O)R, -CO2R, -C(O)N(R)2, -NRC(O)R, and - N(R)2; wherein R2 could also be a sulphide; each R is independently hydrogen, C 1-6 aliphatic, C3-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, sulphur, or a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms selected from nitrogen, oxygen, or sulphur; R3 is Formual (Ia) selected from the group consisting of -OEt, and wherein R5 and R6 are independently selected from the group consisting of H, halide, methoxy, thiomethyl, morpholine and trifluoromethyl;R4 is selected from the group consisting of C1-6-alkyl-, and R4.1-CH2- wherein, R4.1 is C3-6-cycloalkyl-, a 5-6 membered heterocyclic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, sulphur; optionally substituted with one R4.1.1 wherein, R4.1.1 is selected from -H, C1-4-alkyl, optionally substituted with one substituent selected from H2N(O)C- or EtO(O)C-;X is carbon or nitrogen; A is selected from the group consisting of 6 membered unsaturated ring, with 1-3 nitrogen atoms, which is optionally substituted by -NH2,and Formula (Ib), wherein ring B is a fused 5-10 membered saturated or partially unsaturated heterocyclic mono- bicyclic ring having 1-3 heteroatoms selected from nitrogen, oxygen or sulphur, which is optionally substituted by -OH; and m is 1 or 2; and n is 1 or 2.

First Nondiscriminating Translocator Protein Ligands Produced from a Carbazole Scaffold

Development of neuroinflammation agents targeting the translocator protein (TSPO) has been hindered by a common single nucleotide polymorphism (A147T) at which TSPO ligands commonly lose affinity. To this end, carbazole acetamide scaffolds were synthesized and structure activity relationships elaborated to explore the requirements for high-affinity binding to both TSPO wild type (WT) and the polymorphic TSPO A147T. This study reports high binding affinity and nondiscriminating TSPO ligands.

A process for preparing 4 - amino - N - alkyl benzyl amine method

The present invention belongs to an organic intermediate preparation, and particularly relates to a 4-amino-N-alkyl benzylamine preparation method. According to the present invention, N-alkyl benzylamine is adopted as a raw material, acetylation, positioning nitrification and deprotection are performed, and hydrogenation reducing is performed in the presence of a multi-component skeleton Ni-Fe-Cu catalyst, wherein the total yield is more than or equal to 90%; and the method has characteristics of simple process, mild operating conditions and low pollution, the catalyst used in the reaction has high activity and high selectivity, the catalytic hydrogenation selectivity is more than or equal to 99.9%, the yield is more than or equal to 99.9%, the catalyst can be repeatedly applied, and the production cost can be effectively reduced compared with the traditional process.

Exploiting the 4-Phenylquinazoline Scaffold for the Development of High Affinity Fluorescent Probes for the Translocator Protein (TSPO)

The quinazoline class was exploited to search for a new translocator protein (TSPO) fluorescent probe endowed with improved affinity and residence time (RT). Computational studies on an "in-house" collection of quinazoline derivatives, featuring highly st

Structure-activity relationship refinement and further assessment of 4-phenylquinazoline-2-carboxamide translocator protein ligands as antiproliferative agents in human glioblastoma tumors

Structure-activity relationships (SARs) within the 4-phenylquinazoline-2- carboxamide series of translocator protein (TSPO) ligands have been explored further by the synthesis and TSPO binding affinity evaluation of N-benzyl-N-ethyl/methyl derivatives var

8-HETEROARYLPURINE MNK2 INHIBITORS FOR TREATING METABOLIC DISORDERS

This invention relates to 8-Heteroarylpurine Mnk2 Inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.

Substituted indolines which inhibit receptor tyrosine kinases

Indolinones of the formula having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are: (a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone, (b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and (c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.

1,5-benzodiazepine compounds, their production and use

A compound represented by the formula (I) [wherein ring B represents a cyclic hydrocarbon group which may have substituent(s); Z represents hydrogen atom or a cyclic group which may have substituent(s); R1 represents hydrogen atom, a hydrocarbon group which may have substituent(s), a heterocyclic group which may have substituent(s) or an acyl group; R2 represents amino group which may have substituent(s); D represents a bond or a divalent group; E represents a bond, —CO—, —CON(Ra)—, —COO—, —N(Ra)CON(Rb)—, —N(Ra)COO—, —N(Ra)SO2—, —N(Ra)—, —O—, —S—, —SO— or —SO2— (Ra and Rb each independently represents hydrogen atom or a hydrocarbon group which may have substituent(s)); G represents a bond or a divalent group; L represents a bond or a divalent group; A represents hydrogen atom or a substituent; X and Y each represents hydrogen atom or an independent substituent; and . . . represents that R2 and an atom on ring B may form a ring] or a salt thereof, and a process for producing the same.

Substituted indolinones with kinase inhibitory activity

Substituted indolinones of general formula having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: 3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]-5-a