176721-03-2Relevant articles and documents
Preparation method of dexmedetomidine hydrochloride and its intermediate
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Paragraph 0162; 0165, (2018/07/15)
The invention discloses a preparation method of dexmedetomidine hydrochloride and its intermediate. A preparation method of dexmedetomidine L-tartrate comprises the steps of subjecting dexmedetomidineintermediate III and hydrogen to reduction reaction in an organic solvent in the presence of a chiral catalyst, and subjecting the reduced product and tartaric acid to neutralization reaction to obtain dexmedetomidine L-tartrate II, wherein the chiral catalyst is (+)-1,2-bis(2S-5S)-diethylphospholano-benzene(1,5-cyclooctadiene)rhodium trifluoromethanesulfonate. The preparation method herein has ashort step path, has no need for chiral splitting, and has high total molar yield; the product prepared herein has high purity, reaches the standard for bulk pharmaceutical chemicals and is suitablefor industrial production.
Method for preparing dexmedetomidine
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Paragraph 0050; 0051; 0061; 0062; 0063, (2017/01/05)
The invention provides a method for preparing dexmedetomidine, and particularly provides a method for preparing medetomidine midbody 1-(2,3-dimethyl phenyl)-1-(1-trityl-1H-imidazole-4-base) ethyl alcohol. The compound medetomidine midbody as shown in formula I is synthesized through Grignard reaction. The invention further provides a method for preparing dexmedetomidine hydrochloride. The technology has the advantages that the number of steps is small, yield is high, operation is easy, and product purity is high and is quite suitable for industrial production.
Method for preparing medetomidine and its salts
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Page/Page column 6, (2008/12/04)
The invention provides an improved, highly efficient method for preparing Medetomidine, and its salts, in particular its pharmaceutically acceptable salts. The method utilizes the high reactivity of halogenated imidazoles towards transmetalation with Grignard reagents and the subsequent reaction with 2,3-dimethylbenzaldehyde.