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A method for synthesizing loxapine

A technology of compound and iridium complex, which is applied in the field of synthesizing loxapine, can solve the problems of low atom economy and environmental pollution, and achieve the effect of broad development prospects

Active Publication Date: 2022-04-15
NANJING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although the synthetic method of loxapine has been developed, in the original report, the synthetic method uses toxic chemical reagents, multi-step organic reactions, uses organic solvents, has low atom economy, and pollutes the environment

Method used

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  • A method for synthesizing loxapine
  • A method for synthesizing loxapine
  • A method for synthesizing loxapine

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Embodiment 1

[0022] Amoxapine (156.9mg, 0.5mmol), [(Cp*IrCl) 2 (thbpym)][Cl] 2 (2.5mg, 0.0025mmol, 0.5mol%), potassium hydroxide (28mg, 0.5mmol, 1equiv), CH 3 OH (0.5mL), H 2 O (0.5 mL) was sequentially added to a dry 25 mL Kirschner tube, and the reaction mixture was reacted at 130° C. for 12 hours, and then cooled to room temperature. The solvent was removed by rotary evaporation, and then the pure target compound was obtained by column chromatography (developing solvent: petroleum ether / ethyl acetate), yield: 67%. 1 H NMR (500 MHz, CDCl3) δ7.33 (dd, J = 8.7, 2.5 Hz, 1H, ArH), 7.29 (d, J = 2.5 Hz, 1H, ArH), 7.14 (d, J = 8.5 Hz, 2H ,ArH),7.10–7.05(m,2H,ArH),6.99–6.94(m,1H,ArH),3.53(bs,4H,CH2),2.50(bs,4H,CH2),2.33(s,3H, CH3); 13 C NMR (125 MHz, CDCl3) δ 159.1, 158.8, 151.7, 140.0, 132.4, 130.1, 128.9, 127.0, 125.7, 124.9, 124.4, 122.6, 120.0, 54.7, 47.2 (bs), 46.0.

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Abstract

The invention relates to a method for synthesizing loxapine. The steps are: in a reaction vessel, add amoxapine, CH 3 OH, water, iridium complex catalyst and base, after heating and reacting for several hours, cooled to room temperature, spin-dried the solvent, and then separated by column to obtain the target compound. The present invention synthesizes loxapine through the catalysis of metal iridium catalyst, uses amoxapine and methanol to react, and synthesizes in one step. The raw material used in the reaction is a commercial reagent, and the reaction generates water as a by-product, without environmental pollution, and Water should be used as a solvent. Compared with the previous synthesis method using organic matter as a solvent, the present invention is more environmentally friendly and has high atomic economy in reaction.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a method for synthesizing loxapine. Background technique [0002] Loxapine (Loxapine) chemical name: 2-chloro-11-(4-methyl-1-piperazinyl) dibenzo[b,f][1,4]oxazepine, is a neuroleptic neuroleptic antipsychotic drugs. Loxapine can block dopamine D2 receptors; it can also act on other centers including: anticholinergic and α-adrenergic nerve blockade. In the treatment of negative symptoms of schizophrenia, paranoid symptoms and obsessive-compulsive neurosis, the drug has certain advantages. Although the synthetic method of loxapine has been developed, in the original report, the synthetic method uses toxic chemical reagents, multi-step organic reactions, uses organic solvents, has low atom economy, and pollutes the environment. Contents of the invention [0003] The object of the present invention is to provide a method for synthesizing Loxapine. [000...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D267/20
CPCC07D267/20
Inventor 李峰韩兴有孟冲
Owner NANJING UNIV OF SCI & TECH
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