72955-94-3Relevant articles and documents
Method for preparing carvedilol intermediate N-benzyl carvedilol
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Paragraph 0012; 0022; 0023; 0024; 0025; 0026; 0027-0035, (2017/05/23)
The invention relates to a method for preparing a carvedilol intermediate N-benzyl carvedilol, wherein the method comprises the following steps: (1) firstly, loading a compound II, a compound III, sodium hydroxide and a solvent into a reaction kettle, heating up to a reaction temperature, and carrying out a vigorous stirring reaction, to obtain a reaction material liquid; (2) in the reaction process, pumping the reaction material liquid into an external circulation water removal system filled with a water removal agent at a certain flow velocity, and carrying out circulation water removal; and (3) after the reaction is finished, discharging a product I from the bottom of the reaction kettle, and recrystallizing to obtain a compound I. Compared with the prior art, water generated in the nucleophilic substitution reaction of the compound II and the compound III is removed timely by the external circulation water removal system, the conversion rate of the reaction raw materials of the compound II and the compound III is greatly increased, low-energy-consumption, simple and quick continuous production is achieved, the yield of the obtained reaction product I is more than 90%, and the chemical purity is more than 97%.
PROCESS FOR PREPARATION OF 1-(9H-CARBAZOL-4-YLOXY)-3-[[2-(2- METHOXYPHENOXY) ETHYL] AMINO]-2-PROPANOL
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Page/Page column 11-12, (2009/10/22)
The present invention relates to a process for preparation of l-(9H-carbazol-4-yloxy)-3- [[2-(2-methoxyphenoxy) ethyl] amino]-2-propanol and its salts comprising; a)reacting 1- (9H-carbazol-4-yloxy)-3-arylmethylamino-2-propanol or its 9-substituted derivatives with 2-(2-methoxyphenoxy)-haloethane; and b) deprotecting the resulting intermediate to obtain l-(9H-carbazol— 4— yloxy)-3-[[2-(2-methoxyphenoxy)ethyl] amino]-2-propanol in free form or its acid addition salt, which are pharmaceutically valuable compounds.
A PROCESS FOR PREPARATION OF 1-[9H-CARBAZOL-4-YLOXY]- 3-[{2-(2-(-(METHOXY)PHENOXY)-ETHYL}-AMINO]-PROPAN-2-OL
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Page 13; 17-18, (2008/06/13)
The present invention provides a process for preparation of 1-[9H-carbazol-4-yloxy]-3-[{2-(2-(methoxy)phenoxy)-ethyl}-amino]-propan-2-ol, a compound of formula 1 in racemic form or in the form of optically active R or S enantiomer or its pharmaceutically acceptable salt, comprising, reacting 4-(oxiranylmethoxy)-9H-carbazole, a compound of formula (2) or the R or S enantiomer thereof with a compound of formula (5), wherein R1 is benzyl or substituted benzyl group, in an aprotic organic solvent in presence of a catalyst to obtain a compound of formula (6), or the R or S enantiomer thereof, wherein R1 is as defined above. The resultant compound of formula (6) is subjected to debenzylation reaction by catalytic hydrogenation to obtain the compound of formula (1), if desired converting the resultant compound of formula (1) to a pharmaceutically acceptable salt thereof.