102818-67-7

Upstream product

• 102818-66-6 chlormezanone 
• 30897-26-8 2-(4-Chlorophenyl)-3-methyl-3,4,5,6-tetrahydro-2H-1,3-thiazin-4-on 
• 104-88-1 4-chlorobenzaldehyde 
• 102818-66-6 (+)-2-(4-Chlorphenyl)-3-methyl-1,3-thiazinan-4-on-1,1-dioxid 

Downstream Products

• 102818-66-6 (+)-2-(4-Chlorphenyl)-3-methyl-1,3-thiazinan-4-on-1,1-dioxid 
• 77711-05-8 3-sulfinopropionic acid 
• 104-88-1 4-chlorobenzaldehyde 
• 74-89-5 methylamine 
• 102818-66-6 chlormezanone 

Relevant academic research and scientific papers

FURTHER FUNCTIONAL GROUP OXIDATIONS USING SODIUM PERBORATE

Sodium perborate in acetic acid is an effective reagent for the oxidation of aromatic aldehydes to carboxylic acids, iodoarenes to (diacetoxyiodo)arenes, azines to N-oxides, and various types of sulfur heterocycles to S,S-dioxides.Nitriles are unaffected by the reagent in acetic acid, but undergo smooth hydration to amides when aqueous methanol is employed as solvent.

Tranquillizer chlormezanone synthesis method

The invention discloses a tranquillizer chlormezanone synthesis method, which comprises: adding 2-(3-chloro-1,2-dihydroxyphenyl)-3-methyl-1,3-hydrothiazin-4-one and a chloromethyl methyl ether solution to a reaction container, carrying out controlled stirring, controlling the temperature of the solution, adding a 2-methyl-2,4-pentanediol solution, adding potassium ruthenate in batches, and continuously carrying out the reaction; and cooling the solution, adding a potassium carbonate solution in batches, layering the solution, taking out the oil layer, adding a benzenesulfonic acid solution, adjusting the pH value, extracting multiple times with a hexafluorobenzene solution, extracting multiple times with a dimethyl phosphate solution, washing with a 1,2-dibromobenzene solution, re-crystallizing in a polypropylene glycol solution, and dehydrating with a dehydrating agent to obtain the finished product chlormezanone.

New results on the synthesis of the centrally acting muscle relaxant chlormezanone and its resolution on a gram scale using a Chiralcel OD column

2-(4-Chlorophenyl)-4-metathiazanone (2) is the intermediate product for the two step-synthesis of chlormezanone (1), a centrally acting muscle relaxant. The second step includes the oxidation of its sulfur atom. It has been found that the foregoing reacti

Important pharmaceutical-chemical characteristics of the centrally acting muscle relaxant chlormezanone

The enantinomers of chlormezanone (1) may be achieved by enantioselective HPLC separation with a yield of 98% using a OD-Daicel column. Both enantiomers bind to human serum albumin (HSA) at pH 7,4 to a range of 11-12%. Binding to the globuline fractions is much less (2-4%, equilibrium dialysis, validation by ultrafiltration). It could be demonstrated by means of 1H-NMR spectroscopy that 1 binds to HSA with the benzene ring as well as with the thiazanone ring. The velocity of racemisation could be measured for the first time using a BSA column. The enantiomers undergo racemisation at pH 7.4 and 37 °C with a halflife of approx. 20.5 h.

Water dispersion containing ultrafine particles of organic compounds

A water-dispersible condensate of water-insoluble ultrafine particles of medicine or hormones having a particle size of at largest 4 μm prepared by the steps of heating the medicine or hormone in a vacuum vessel at a temperature of 30° C. higher than the boiling point and at a pressure between 0.01 Torr and 10 Torr to evaporate the medicine or hormone and condensing the medicine or hormone on a recovery plate to obtain the condensate.

Chromatographic Resolution of the Drug Chlormezanone and of Some Structural Analgues

The racemic drug chlormezanone (1a) is resolved into the enantiomers by HPLC on cellulose triacetate and the silica gel-bound phenylalanine polymer 2b.By preparative column chromatography on cellulose triacetate, both enantiomers were obtained on gram scale.Their racemization rate was determined as a function of the pH value.Furthermore, on cellulose triacetate and on polyamides of type 2 and 3a-d, structure analogues of chlormezanone were separated into enantiomers, some of them completely.