56233-10-4

Upstream product

• 55-86-7 mechlorethamine hydrochloride 
• 140-29-4 phenylacetonitrile 
• 109-01-3 1-methyl-piperazine 
• 103-63-9 1-phenyl-2-bromoethane 
• 100-42-5 styrene 
• 1015484-22-6 1-methyl-4-((trifluoro-λ⁴-boranyl)methyl)piperazine potassium 
• 100-44-7 benzyl chloride 

Relevant academic research and scientific papers

A potassium magnesiate complex: Synthesis, structure and catalytic intermolecular hydroamination of styrenes

A new heterobimetallic potassium magnesiate complex KMg[N(SiMe3)2]2Bn (Bn = PhCH2-) was synthesized by simply mixing magnesium amide and potassium benzyl in toluene. The TMEDA-ligated potassium magnesiate comple

Synthesis of Arylethylamines via C(sp3)-C(sp3) Palladium-Catalyzed Cross-Coupling

Substituted arylethylamines represent a key structural motif in natural, pharmaceutical, and agrochemical compounds. Access to such scaffolds has been the subject of long-standing synthetic interest. Herein, we report the synthesis of such scaffolds via a palladium-catalyzed C(sp3)-C(sp3) coupling between (chloromethyl)aryls and air-/moisture-stable N,N-dialkylaminomethyltrifluoroborate salts. Rapid hit identification was achieved using microscale high-throughput experimentation and was followed by millimolar-scale reaction parameter optimization. A range of structurally and electronically varied arylethylamine products were obtained in moderate to excellent yields (27-96%, >60 examples). The reaction mechanism is proposed to proceed via formation of a trialkylbenzylammonium species prior to oxidative addition.

Lithium-Catalyzed anti-Markovnikov Intermolecular Hydroamination Reactions of Vinylarenes and Simple Secondary Amines

Various β-arylethylamine derivatives were straightforwardly obtained by the lithium-catalyzed anti-Markovnikov selective intermolecular hydroamination reaction of secondary aliphatic amines with vinylarenes. The use of only 1.5 mol % LiCH2TMS as a solid base in THF proved to be efficient to deliver the target products at room temperature with up to complete conversions. Both reaction partners were, moreover, used in equivalent amounts; thus, this protocol best respects the concepts of sustainable chemistry for the easy preparation of lead structures for pharmaceutically active compounds.

Anti-markovnikov hydroamination of aromatic alkenes with secondary amines catalyzed by easily accessible yttrium complexes

Binaphthylamido alkyl yttrium complexes have been proven to promote the anti-Markovnikov addition between various styrene derivatives and secondary amines efficiently. Although the reaction has to be performed at high temperature, it is realized advantage

Synthesis of β-phenylethylamines from styrene derivatives

β-Phenylethylamines are prepared from the styrene derivatives; 4,4- dimethyl-2-(2-vinylphenyl)-2-oxazoline, 2-(3-methoxy-2-vinylpnenyl)-4,4- dimethyl-2-oxazoline, 2-vinylbenzoic acid, styrene, β-methylstyrene, and α- methylstyrene.

Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists

Several alkylpiperazines, monocyclic subfragments of known tricyclic neuroleptic agents, were evaluated as dopamine antagonists in the isolated rabbit ear artery preparation. Compounds prepared and evaluated are of the general structure Ar-X-(CH2)(n)-Y, where X = C, O, and N, n = 1-3, and Y, for the most part, was 4-methylpiperazine. Those compounds where X = NH, n = 3, and X = (Z)-CH=CH, n = 2, with an electron-witdrawing group meta to the side chain, possess dopamine antagonist activity comparable to that of clozapine. It is concluded that the entire tricyclic structure of phenothiazine-like agents (or at least more than a monocyclic ring system) is necessary for optimal activity as a dopamine antagonist in the receptor preparation used in this study.