52437-65-7

Upstream product

• 42013-66-1 dezocine hydrobromide 
• 50666-38-1 4-Methoxy-1-methyl-tricyclo[7.5.1.0^2,7]pentadeca-2,4,6-trien-15-one oxime 
• 1204-23-5 1-methyl-7-methoxy-2-tetralone 
• 131434-57-6 (R)-(+)-7-methoxy-1-(5'-bromopentyl)-1-methyl-2-tetralone 
• 42263-97-8 (1R,9S)-4-Methoxy-1-methyl-tricyclo[7.5.1.0^2,7]pentadeca-2,4,6-trien-15-one oxime 
• 42264-11-9 (5R,11S,13S)-3-methoxy-5-methyl-5,6,7,8,9,10,11,12-octahydro-5,11-methylenebenzocyclodecene-13-amine 

Relevant academic research and scientific papers

Dezocine production process

The invention provides a dezocine production process, and relates to the technical field of medical chemistry. The dezocine production process comprises the following steps of 1) synthesis of dezocine ammonium salt, 2) synthesis of methyl dezocine salt, 3) synthesis of a crude dizocine product and 4) refining and packaging of the crude dizocine product. By means of the four processes of synthesis of dezocine ammonium salt, synthesis of methyl dezocine salt, synthesis of the crude dizocine product and refining and packaging of the crude dizocine product, the synthesis steps and the reaction conditions are optimized, the synthesis cycle is shortened, and meanwhile the detailed processes of the synthesis of dezocine ammonium salt, synthesis of methyl dezocine salt, synthesis of the crude dizocine product and refining of the crude dizocine product are described in details; key process parameters and product quality standards are defined, thus the dezocine production process can rapidly grasp key control points, and the synthesis reaction can be helped to be conducted efficiently and stably.

Enantioselective phase-transfer catalyzed alkylation of 1-methyl-7-methoxy-2-tetralone: An effective route to dezocine

In order to prepare asymmetrically (R)-(+)-1-(5-bromopentyl)-1-methyl-7-methoxy-2-tetralone (3a), a key intermediate of dezocine, 17 cinchona alkaloid-derived catalysts were prepared and screened for the enantioselective alkylation of 1-methyl-7- methoxy-2-tetralone with 1, 5-dibromopentane, and the best catalyst (C7) was identified. In addition, optimizations of the alkylation were carried out so that the process became practical and effective.

DEZOCINE ANALOGUE

Disclosed in the present invention is a Dezocine analogue, and particularly disclosed are compounds represented by formula (I), (II) and (III), a pharmaceutically acceptable salt or tautomer thereof.

Combination of selected opioids with muscarine antagonists for treating urinary incontinence

Active compound combinations of compounds of group A, particularly opioids, and compounds of group B, particularly anti-muscarine agents and other substances suitable for treatment of an increased urge to urinate or urinary incontinence. Related pharmaceutical formulations and methods of treatment of an increased urge to urinate or urinary incontinence are also provided.

Asymmetric alkylation of α-aryl substituted carbonyl compounds by means of chiral phase transfer catalysts. Applications for the synthesis of (+)-podocarp-8(14)-en-13-one and of (-)-Wy-16,225, a potent analgesic agent

Asymmetric induction in the alkylation (alkyl halides and enones) of α-aryl substituted ketones, esters and lactones by means of CPTC has been evaluated. The catalysts used are the bromides of N-(p-trifluoromethyl) benzyl derivatives of cinchonine, cinchonidine, dihydrocinchonine and dihydrocinchonidine. The potential of the method is illustrated by the asymmetric synthesis of (+)-podocarp-8(14)-ene-13-one (13) and of (-)-Wy-16,225 (10), a bridged aminotetralin with potent analgesic properties.