- Synthesis method of 4-aminomethylisoxazole
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The invention discloses a synthesis method of 4-aminomethylisoxazole, which comprises the following steps: carrying out a reaction on N,N-dimethylformamide, bromoacetic acid and phosphorus oxychlorideto obtain fluoroborate, then adding fluoroboric acid and hydroxylamine hydrochloride to obtain isoxazole 4-formaldoxime, and finally preparing the 4-aminomethyl isoxazole under the catalytic action of aluminum amalgam. The method has the advantages that the raw material synthesis difficulty is low, the purification process is simple, the synthesis method also has the advantages of simple operation, high efficiency and low raw material cost, and the synthesis route has the advantages of simple and convenient process and suitability for large-scale production in factories.
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Paragraph 0027-0035
(2020/02/14)
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- Regioisomeric 3-, 4- and 5-aminomethyl isoxazoles: Synthesis and muscarinic activity
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A series of 3-, 4- and 5-aminomethyl isoxazoles and isoxazoles with one or two additional methyl groups at the heterocycle were synthesized in order to investigate the structural requirements, ie heterocyclic moiety, regiochemistry and length of an aminoalkyl unit, for muscarinic activity. This was assayed on isolated rabbit vas deferens (M1 receptor subtype) and isolated guinea-pig atrium (M2 receptor subtype) and ileum (M3 receptor subtype). The isoxazoles tested are one to three orders of magnitude less active than furane or oxadiazole derivatives, having similar structural characteristics except for the heterocycle. Thus, the differences in molecular point charges and charge distribution contribute to the muscarinic activity of these compounds more than small differences in molecular shape and conformational energies.
- Dannhardt,Kiefer,Lambrecht,Laufer,Mutschler,Schweiger,Striegel
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p. 839 - 850
(2007/10/03)
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