38430-03-4

Upstream product

• 93-98-1 N-phenyl benzoyl amide 

Downstream Products

• 50655-47-5 Phenyl-[1-phenyl-hept-2-yn-(E)-ylidene]-amine 
• 52687-31-7 1,1,1-Trifluor-2,2-bis(trifluormethyl)-3-phenyl-3-(phenylimino)propan 
• 113396-22-8 α-phenyliminobenzyl 3-pyridyl ether 
• 75029-44-6 1,3-dimethyl-5-benzoylpyrimidine-2,4(1H,3H)-dione 
• 3393-96-2 p-nitrobenzanilide 
• 728-90-5 N-(2-nitrophenyl)benzanilide 
• 185106-85-8 N-[(Z)-2-(4,5-dihydro-1,3-oxazol-2-yl)-1-phenylethenyl]aniline 
• 185107-18-0 [(Z)-2-(4,5-Dihydro-oxazol-2-yl)-1-phenyl-propenyl]-phenyl-amine 
• 92566-52-4 ethyl 2-phenylquinazoline-4-carboxylate 
• 82483-97-4 (Rs)-2-(Z)-phenylimino-2-phenylethyl-1-p-tolylsulfoxide 
• 2556-46-9 N,N'-diphenylbenzenecarboximidamide 
• 20800-34-4 N-(N-Phenyl-benzimidoyl)-N'-phenyl-thioharnstoff 
• 70375-39-2 1-methyl-3-[(phenyl)-(phenylimino)methyl]thiourea 
• 871667-88-8 ethyl 1,2-diphenyl-4-[1-phenyl-1-(phenylamino)methylidene]-4,5-dihydro-5-oxopyrrole-3-carboxylate 

Relevant academic research and scientific papers

Palladium-catalyzed synthesis of α-iminoamides from imidoyl chlorides and a carbamoylsilane

A series of pure imidoyl chlorides were converted into α-iminoamides by treatment with a carbamoylsilane under catalysis by palladium(0) complexes.

One-pot synthesis of polyfunctionalized quinolines: Via a copper-catalyzed tandem cyclization

An efficient one-pot approach for the synthesis of polyfunctionalized quinolines was developed via a sequence of copper-catalyzed coupling reaction/propargyl-allenyl isomerization/aza-electrocyclization. Easily available starting materials, mild conditions, and a wide substrate scope make this approach potentially useful.

Amidinyl Radical Formation through Anodic N?H Bond Cleavage and Its Application in Aromatic C?H Bond Functionalization

We report herein an atom-economical and sustainable approach to access amidinyl radical intermediates through the anodic cleavage of N?H bonds. The resulting nitrogen-centered radicals undergo cyclizations with (hetero)arenes, followed by rearomatization,

Rhenium-catalyzed synthesis of 3-imino-1-isoindolinones by C-H bond activation: Application to the synthesis of polyimide derivatives

Polyimide solution: Synthesis of the title compounds from aromatic imidates and isocyanates in good to excellent yields by a rhenium-catalyzed C-H bond transformation is described. The reaction also proceeded in high yield on gram scale and could be applied to the synthesis of polyimide derivatives (see figure), which are highly soluble in organic solvents. Copyright

Discovery of an orally available, brain penetrant BACE1 inhibitor that affords robust CNS Aβ reduction

Inhibition of BACE1 to prevent brain Aβ peptide formation is a potential disease-modifying approach to the treatment of Alzheimer's disease. Despite over a decade of drug discovery efforts, the identification of brain-penetrant BACE1 inhibitors that substantially lower CNS Aβ levels following systemic administration remains challenging. In this report we describe structure-based optimization of a series of brain-penetrant BACE1 inhibitors derived from an iminopyrimidinone scaffold. Application of structure-based design in tandem with control of physicochemical properties culminated in the discovery of compound 16, which potently reduced cortex and CSF Aβ40 levels when administered orally to rats.

One-pot synthesis of 2-imidazolines via the ring expansion of imidoyl chlorides with aziridines

We herein report a simple and convenient one-pot synthesis of highly substituted 2-imidazolines in a regiocontrolled and stereospecific matter through the ring expansion reaction of an imidoyl chloride with an aziridine, analogous to the Heine reaction.

Synthetic studies related to diketopyrrolopyrrole (DPP) pigments. Part 3: Syntheses of tri- and tetra-aryl DPPs

Novel synthetic methodologies leading towards 2,3,5-triaryl- and 2,3,5,6-tetraaryl-2,5-dihydropyrrolo[3,4-c]pyrrole-1,4-diones (tri- and tetra-aryl-DPPs) and their derivatives have been investigated. Direct arylation of 3,6-diphenyl-DPP was possible using

Selenium-containing heterocycles from isoselenocyanates: Synthesis of 1,3-selenazoles from N-phenylimidoyl isoselenocyanates

The reaction of N-phenylbenzamides 5 with excess SOCl2 under reflux gave N-phenylbenzimidoyl chlorides 6, which, on treatment with KSeCN in acetone, yielded imidoyl isoselenocyanates of type 2. These products, obtained in almost quantitative yield, were stable in the crystalline state. They were transformed into selenourea derivatives 7 by the reaction with NH3, or primary or secondary amines. In acetone at room temperature, 7 reacted with activated bromomethylene compounds such as 2-bromoacetates, acetamides, and acetonitriles, as well as phenacyl bromides and 4-cyanobenzyl bromide to to give 1,3-selenazol-2-amines of type 9 (Scheme 2). A reaction mechanism via alkylation of the Se-atom of 7, followed by ring closure and elimination of aniline, is most likely (cf. Scheme 7). In the case of selenourea derivatives 7d and 7I with an unsubstituted NH2 group, an alternative ring closure via elimination of H2O led to 1,3-selenazoles 10a and 10b, respectively (Schemes 4 and 7). On treatment with NaOH, ethyl 1,3- selenazole-5-carboxylates 9I and 9s were saponified and decarboxylated to give the corresponding 5-unsubstituted 1,3-selenazoles 12a and 12b (Scheme 6). The molecular structures of selenourea 7f and the 1,3-selenazoles 9c and 9d have been established by X-ray crystallography (Figs. 1 and 3).

Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework

A novel class of potent and selective non-peptide neurokinin-3 (NK-3) receptor antagonists, featuring the 4-quinolinecarboxamide framework, has been designed based upon chemically diverse NK-1 receptor antagonists. The novel compounds 33-76, prompted by chemical modifications of the prototype 4, have been characterized by binding analysis using a membrane preparation of chinese hamster ovary (CHO) cells expressing the human neurokinin-3 receptors (hNK-3-CHO), and clear structure-activity relationships (SARs) have been established. From SARs, (R)-N-[α-(methoxycarbonyl)benzyl]-2- phenylquinoline-4-carboxamide (65, SB 218795, hNK-3-CHO binding K(i) = 13 nM) emerged as one of the most potent compounds of this novel class. Selectivity studies versus the other neurokinin receptors (hNK-2-CHO and hNK-1-CHO) revealed that 65 is about 90-fold selective for hNK-3 versus hNK-2 receptors (hNK-2-CHO binding K(i) = 1221 nM) and over 7000-fold selective versus hNK-1 receptors (hNK-1-CHO binding K(i) = >100 μM). In vitro functional studies in rabbit isolated iris sphincter muscle preparation demonstrated that 65 is a competitive antagonist of the contractile response induced by the potent and selective NK-3 receptor agonist senktide with a K(b) = 43 nM. Overall, the data indicate that 65 is a potent and selective hNK-3 receptor antagonist and a useful lead for further chemical optimization.