- Preparation method of benzphetamine hydrochloride
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The invention relates to the field of chemical pharmacy, and in particular relates to a preparation method of benzphetamine hydrochloride. According to the method, the use of controlled products suchas ephedrine, pseudoephedrine, deoxyephedrine and the like is avoided; the raw materials are cheap and easy to obtain, so that the synthesis cost is reduced; by using the preparation method disclosedby the invention, the high-purity target compound can be obtained at high yield, and industrial large-scale production is easy.
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Paragraph 0071-0073; 0080-0085
(2020/01/25)
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- Investigation of a flexible enantiospecific approach to aziridines
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(Chemical Equation Presented) A flexible approach to functionalized and enantioenriched aziridines has been developed from an intermediate aziridinylmethyl tosylate. This protocol features a Cu-catalyzed Grignard substitution reaction that allows a range of functionalized organic fragments to be incorporated. Moreover, a convenient one-pot procedure is outlined that allows the trityl group to be exchanged for a range of common N-protecting groups.
- Jamookeeah, Clare E.,Beadle, Christopher D.,Jackson, Richard F. W.,Harrity, Joseph P. A.
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p. 1128 - 1130
(2008/09/18)
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- A new and expeditious asymmetric synthesis of (R)- and (S)-2-aminoalkanesulfonic acids from chiral amino alcohols
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The mechanism for the transformation of β-amino alcohol methanesulfonate hydrochlorides into sodium β-amino alkanesulfonates using sodium sulfite was investigated. The results show that sodium sulfite initially neutralizes the β-amino alcohol methanesulfonate hydrochloride to give a free β-amino alcohol methanesulfonate, which then cyclizes to a 2-alkylaziridine. Attack by the previously formed sodium bisulfite at the less hindered carbon atom of the aziridine ring then yields a β-amino alkanesulfate sodium salt. Based on this mechanistic proposal, a new and rapid asymmetric synthesis of (R)- and (S)-2-aminoalkanesulfonic acids from chiral amino alcohols was developed. Chiral amino alcohols were converted to chiral aziridines through the Wenker method or Mitsunobu reaction and the resulting aziridines were reacted with sodium bisulfite to produce chiral β-amino alkanesulfonic acids.
- Xu, Jiaxi
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p. 1129 - 1134
(2007/10/03)
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- Deprotection of sulfonyl aziridines
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The deprotection of the chiral N-sulfonyl aziridines 1-3 has been studied under different desulfonylation conditions. Two methods for the efficient aleprotection of 2-benzyl-, 2-phenyl-, and 2-carboxyl-N- sulfonylaziridines were found. The desulfonylation with lithium and a catalytic amount of di-tert-butyl biphenyl in THF at -78 °C led to the corresponding NH aziridines with yields up to 85%. Alternatively, the desulfonylation could be carried out with magnesium in methanol under ultrasonic conditions. The latter proved to be a very mild method and afforded the desulfonylated aziridines with yields up to 75%, even when the 2-phenyl substituted aziridine 2 was the studied substrate. Furthermore, in all the cases studied, no racemization was observed in the chiral center of the aziridines.
- Alonso, Diego A.,Andersson, Pher G.
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p. 9455 - 9461
(2007/10/03)
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