1461-82-1Relevant academic research and scientific papers
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.
Process for the preparation of pure, unsymmetrically disubstituted ureas
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, (2008/06/13)
Process for the preparation of pure, unsymmetrically disubstituted ureas of the general formula STR1 in which R denotes a phenyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy, aryloxy or trifluoromethyl groups, an oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, benzoxazolyl or benzothiazolyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy or trifluoromethyl groups and R1 and R2 independently of one another denote a hydrogen atom or an alkyl group, where R1 and R2 are not simultaneously hydrogen or R1 and R2 together denote a butylene or pentylene group, by reaction of an N-alkyl- or N,N-dialkylurea with an unsubstituted or substituted arylamine or a heterocyclic amine in the presence of that amine which is already present in the starting material, the respective N-alkyl- or N,N-dialkylurea.
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
