1461-82-1Relevant articles and documents
Synthesis method of celiprolol drug intermediate 3-(4-enthoxyphenyl)-1,1-diethylurea
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Paragraph 0015; 0016, (2016/11/17)
A synthesis method of celiprolol drug intermediate 3-(4-enthoxyphenyl)-1,1-diethylurea comprises steps as follows: 0.22 mol of p-phenetidine, 0.45-0.47 mol of sodium hydrogen sulfite and 80-90 ml of tetrahydrofuran are added to a reaction container provided with a stirrer and a dropping funnel, the stirring speed is controlled within 130-160 rpm, the solution temperature is controlled within 35-40 DEG C, 0.25-0.27 mol of N,N-diethylamino formamide is dropwise added, the addition time is controlled within 4-5 h, the solution is stirred continuously to react for 30-35 h, 300-350 ml of a sodium chloride solution is added, the pH of the solution is adjusted to range from 4 to 5 with an oxalic acid, the solution reacts continuously for 4-5 h, solids are separated out, the solution is cooled to the temperature of 10-15 DEG C, filtration, washing with a salt solution, dehydration with a dehydrating agent and recrystallization in hexane are performed, and 3-(4-enthoxyphenyl)-1,1-diethylurea is obtained.
On the Synthesis of Cardioselective β-Adrenergic Receptor Blocking Agent Celiprolol
Zoelss, G.
, p. 2 - 4 (2007/10/02)
The synthesis of 3--1,1-diethyl-urea-hydrochloride (celiprolol-HCl, in the following briefly called celiprolol; ST 1396-HCl), as well as some physicochemical properties and spectroscopic data are reported. - Key words: β-Blockers; Celiprolol, cardioselectivity, synthesis; ST 1396-HCl