- Preparation method of 4-morpholinyl-2-ethylpiperazine
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The invention discloses a preparation method of 4-morpholinyl-2-ethylpiperazine. The method comprises the following steps: (1) putting 2-hydroxyethylpiperazine and thionyl chloride into a first solvent, and performing a reaction to convert hydroxyl groups into chlorine to obtain a first reaction product; (2) putting the first reaction product obtained in step (1) and boc anhydride into a second solvent, and performing a reaction to obtain an N-boc protected second reaction product; (3) putting the second reaction product obtained in step (2), morpholine and an acid-binding agent into a third solvent at 20-50 DEG C, and performing a reaction to obtain a third reaction product; and (4) dissolving the third reaction product obtained in step (3) and an alkali in a fourth solvent, heating the obtained solution to 40-80 DEG C, performing a reaction for about 10-20 h, concentrating the obtained reaction solution, and extracting and concentrating the obtained concentrate to obtain the 4-morpholinyl-2-ethylpiperazine. Raw materials used in the method are cheap and are easy to obtain, the operation process is simple, and the purity of the obtained product is high and exceeds 99%.
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Paragraph 0052-0053; 0057-0058; 0062-0063
(2020/03/25)
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- Microwave-assisted solvent-free synthesis of 3-[(4-substituted piperazin-1-yl)alkyl] imidazo[2,1-b][1,3]benzothiazol-2(3H)-ones as serotonin3 (5-HT3) receptor antagonists
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A series of novel 3-[(4-substituted piperazin-1-yl)alkyl]imidazo[2,1-b][1, 3]benzothiazol-2(3H)-ones were prepared by microwave irradiation using alumina as solid support and also by a conventional method. The compounds were characterized by spectral data and the purity was ascertained by microanalysis. The synthesized compounds were evaluated for 5-hydroxytryptamine3 antagonisms in a longitudinal muscle-myenteric plexus preparation from guinea pig ileum against the 5-hydroxytryptamine3 agonist, 2-methyl-5-hydroxytryptamine. Among the test compounds, 3-[2-(4-methylpiperazin- 1-yl)ethyl]imidazo[2,1-6][1,3]benzothiazol-2(3H)-one (3b) showed most favorable 5-hydroxytryptamine3 antagonism (pA2 6.7) in the isolated guinea pig ileum.
- Mahesh,Venkatesha Perumal,Pandi
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p. 411 - 414
(2007/10/03)
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