6266-35-9

Upstream product

• 75-55-8 2-Methylaziridine 
• 78-96-6 3-amino-2-propanol 

Downstream Products

• 285125-40-8 2-(2-methyl-4-nitrophenylimino)-5-methyl-1,3-thiazolidine 
• 391668-76-1 1-(3-[1,3]dioxolan-2-ylphenyl)azetidine 
• 2258-21-1 3-(2-methyl-1H-imidazol-1-yl)propan-1-amine 
• 591733-72-1 (4R,5S)-(+)-4-methyl-5-phenyloxazolidin 
• 1005-04-5 4-(2-amino-1-methylethyl)morpholine 
• 54151-70-1 1-(2-aminoisopropyl)-piperidine 
• 50998-07-7 2-Pyrrolidin-1-yl-propylamine 
• 29670-17-5 1-(4-chlorophenylthio)-2-propanamine hydrochloride 
• 104864-10-0 2-(4-chlorophenylthio)propanamine hydrochloride 

Relevant academic research and scientific papers

Substituted 2-arylimino heterocycles and compositions containing them, for use as progesterone receptor binding agents

This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones, 2-arylimino-1,3-thiazolidin-5-ones, and 2-arylimino-1,3-oxazolidines, and their use in modulating progesterone receptor mediated processes, and pharmaceutical compositions for use in such therapies.

2-(Arylthio)ethanamines and &α-(Arylthio)propionamides with Antidepressant Activity

Reaction of aziridine with thiophenols affords 2-arylthioethanamines; with 2-methylaziridine, ring opening occurs regiospecifically to provide 1-arylthio-2-propanamines.The structure of one member of this group, 1-(4-chlorophenylthio)-2-propanamine (7), has been proved by other unambiguous syntheses. 7 and isomer 12 arise from the alkylation of 4-chlorothiophenol with 2-chloropropylamine as well as from the displacement of the tosyl group in 1-(4-chlorophenylthio)-2-tosyloxypropane (13).Alkylation of 4-chlorothiophenol with α-chloropropionamide affords 11 which leads to 12 on LAH reduction.Ethanamines and propanamines are converted into guanidines, amides, ureas and thioureas.Many arylthioethanamines, e.g. 7, 22, 28, 38 and 39 (as HCl salts) and α-arylthiopropionamides, e.g. 11, 86, 91, 93 and 96 exhibit good activity in the DOPA potentiation and reserpine antagonism tests.Among these, 7 HCl is the most potent and does not inhibit rat brain MAO activity.In clinical trials, C 2998-Go compares favourably with imipramine.

Determination des pKa et reaction d'ouverture acide de quelques alkyl-2 et aryl-2 aziridines

Some 2-para substituted aryl aziridines (with pY = CH3O-, CH3-, H-, and Cl-) have been prepared.Their ring opening reaction in acidic medium has been studied and compared with those of two aliphatic aziridines : 2 methyl- and 2,2 dimethyl-aziridine.In aqueous solvent, the addition of HCl, HBr, and HI to the aromatic aziridines leads exclusively to the secondary halogen product, due to the nucleophilic attack on the benzylic carbon.The hydrolysis reaction competes with the addition reaction and is very important for the para methoxy 2-phenyl aziridine.In ethyl alcohol (anhydrous solvent), the hydrohalogenation reaction leads exclusively to halogeno amine with a secondary halogen.The solvolysis reaction, leading to amino-ether, is far less important than in water (excepted for the para methoxy 2-phenyl aziridine).In both solvents, the importance of the solvolysis depends on the HX concentration, as well as the nucleophilic strength of the halogen.The pKa values of these aziridines have been measured, as well as those of 2-phenyl 1-amino 2-ethanol.A linear plot is obtained for the pKa versus ?+p of Brown ; the slopes are respectively -2.8 and 0.Therefore the aromatic aziridines seem to have a behavior similar to that of anilines.