1215194-08-3Relevant articles and documents
Synthesis method of chiral compound
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Paragraph 0151-0152, (2020/01/25)
The invention belongs to the technical field of chemical synthesis, and relates to a synthetic method of a chiral compound, in particular to a synthetic method of (1R, 2S)-1-phenyl-2-(pyrrolidine-1-yl) propan-1-ol. According to an ingenious synthesis strategy, asymmetric reduction can be realized during carbonyl reduction, and a target compound can be directly obtained at high yield. The problem that a target compound cannot be obtained at high yield through asymmetric reduction in the prior art is solved. Moreover, the synthesis of a high-purity compound (A) can be realized by using cheap hydrochloric acid and zinc chloride; in addition, no isomer is wasted; and according to the method, the use of norephedrine controlled product is avoided; the raw materials are cheap and easy to obtain,so that the synthesis cost is reduced; moreover, the preparation method disclosed by the invention is easy for industrial large-scale production.
A (S)- N - methoxy - methyl -2 - (tetrahydro-pyrrolyl) propionamide and its preparation method and application
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Paragraph 0049; 0050, (2017/08/25)
The invention discloses a (S)-N-methoxy-methyl-2-(pyrrolidine) propionamide shown as a formula (5). A preparation method is as follows: subjecting a starting material L-alanine to amino protection, reaction with N,O-dimethyl hydroxylamine hydrochloride, removal of amino protecting group, and alkylation; and subjecting the prepared compound shown as (5) to addition elimination and reduction to obtain an Efavirenz chiral ligand shown as the formula (7). The synthetic method of Efavirenz chiral ligand provided by the invention has the advantages of mild reaction conditions, simple operation, high yield and low production cost, and is suitable for industrialized production.
Chiral separation of cathinone and amphetamine derivatives by HPLC/UV using sulfated β-cyclodextrin as chiral mobile phase additive
Taschwer, Magdalena,Seidl, Yvonne,Mohr, Stefan,Schmid, Martin G.
, p. 411 - 418 (2014/08/05)
In the last years the identification of new legal and illegal highs has become a huge challenge for the police and prosecution authorities. In an analytical context, only a few analytical methods are available to identify these new substances. Moreover, many of these recreational drugs are chiral and it is supposed that the enantiomers differ in their pharmacological potency. Since nonenantioselective synthesis is easier and cheaper, they are mainly sold as racemic mixtures. The goal of this research work was to develop an inexpensive method for the chiral separation of cathinones and amphetamines. This should help to discover if the substances are sold as racemic mixtures and give further information about their quality as well as their origin. Chiral separation of a set of 6 amphetamine and 25 cathinone derivatives, mainly purchased from various Internet shops, is presented. A LiChrospher 100 RP-18e, 250 x 4 mm, 5 μm served as the stationary phase. The chiral mobile phase consisted of methanol, water, and sulfated β-cyclodextrin. Measurements were performed under isocratic conditions in reversed phase mode using UV detection. Four model compounds of the two substance classes were used to optimize the mobile phase. Under final conditions (methanol:water 2.5:97.5 + 2% sulfated β-cyclodextrin) enantiomers of amphetamine and five derivatives were baseline separated within 23 min. In all, 17 cathinones were completely or partially chirally separated. However, as only 3 of 25 cathinones were baseline resolved, the application of this method is limited for cathinone analogs. Additionally, the results were compared with an RP-8e column. Copyright
