1693-66-9

The invention provides an improved synthetic method of (R)-1-aryl-2-propylamine. The improved synthetic method comprises the following steps of: adopting 1-arylacetone as a raw material, adding (R)-1-phenylethylamine, carrying out reductive amination reaction with hydrogen under a common action of a Lewis acid additive and a transitional metal hydrogenation catalyst; carrying out Pd/C catalytic hydrogenation on an obtained intermediate to remove phenethyl on nitrogen and thus obtaining (R)-1-aryl-2-propylamine. The improved synthetic method provided by the invention has the beneficial effectsthat the operation is simple, the adopted Lewis acid additive is low in cost and easy in obtaining, the yield and the enantioselectivity of a product are high, and the application value for industrialsynthesis of (R)-1-aryl-2-propylamine is very high.

Both enantiomers of several phenylethylamines, structurally related to amphetamine, have been prepared in good yields and excellent enantiomeric purity by enzymatic kinetic resolution using CAL-B and ethyl methoxyacetate as the acyl donor. In the case of the 4-hydroxyderivative of amphetamine (compound 4i), the S enantiomer racemized possibly in a dynamic kinetic resolution (DKR) under the enzymatic conditions used. The Royal Society of Chemistry 2011.

Micriorganisms which hydrogenate 2-nitro-1-phenyl-1-propene were screend in type cultures and soil samples.Some actinomycetes belonging to Rhodococcus, Nocardia and Mycobacterium asymmetrically reduced the substrate and gave optically active 2-nitro-1-phenylpropane.Among them, Rhodococcus rhodochrous IFO 3338 gave the best results.The satureted compound was obtained quantitatively, when cultivation was carried out for 3 days at 30 oC with a substrate concentration of 0.4percent.The optical purity of the product was seriously affected by the pH of the medium.The more acidic the medium, the higher the enantiomeric excess.The results suggested that non-enzymatic racemization of the product take place even under neutral conditions.Other substrates, such as 2-nitro-1-propene were also converted to optically active 2-nitro-1-substituted propane.