1908-84-5Relevant articles and documents
Preparation method of 2-methylaziridine
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Paragraph 0024; 0030-0034; 0038; 0044-0047; 0050; 0056-0060, (2019/07/29)
The invention belongs to the field of chemical synthesis, and particularly relates to a preparation method of 2-methylaziridine. The 2-methylaziridine is synthesized from isopropanolamine, sulfuric acid and liquid caustic soda as raw materials, the synthesis condition is mild, and mass industrial production is facilitated. Besides, the synthesis materials are simple, sulfate esterification and liquid caustic soda hydrolysis are adopted, caustic soda flakes are used for purification in the distillation and purification process, few byproducts are produced, and the method is green and environmentally friendly; initial distillation under normal pressure and fine distillation under low pressure are adopted, and the obtained 2-methylaziridine has the purity of 99% or above.
Synthesis and Biological Activity of 2-Aminothiazolines and 2-Mercaptothiazolines as Octopaminergic Agonists
Hirashima, Akinori,Yoshii, Yutuka,Eto, Morifusa
, p. 2537 - 2546 (2007/10/02)
2-Aminothiazoline derivatives were synthesized by both hydrochloric acid-catalyzed cyclization of thiourea and cyclization of β-aminoalkyl hydrogen sulfate with isothiocyanate in the presence of sodium hydroxide.Substituted 2-mercaptothiazoline derivatives were prepared by alkylation or acylation of the sodium salt of 2-mercaptothiazoline, which was obtained from β-aminoalkyl hydrogen sulfate with carbon disulfide. 2-(4-Chloro-o-toluidino)-2-thiazoline (III-16) was 33percent as effective as octopamine at 100 μM in stimulating adenylate cyclase of Periplaneta americana ventral-nerve-cord homogenates.Its activity was nonadditive to the activity of octopamine.Stimulation of nerve-cord adenylate cyclase activity by III-16 was inhibited by several antagonists, including mianserin, cyproheptadine, chlorpromazine and gramine.The rank-order ability of these antagonists to block the activation by III-16 was identical to the rank-order ability of the same antagonists to block enzyme activation of octopamine.The β-adrenergic antagonist propanolol was less potent.These data suggest that III-16 is a potent and selctive agonist of octopamine-activated adenylate cyclase.Aminothiazolines which activated adenylate cyclase by 10-87percent relative to octopamine also had acaricidal activity at 300 ppm, indicating a correlation between the in vitro octopaminergic-agonist activity and in vivo acaricidal activity of aminothiazolines.
