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Preparation method of asenapine

A compound, red aluminum technology, applied in the field of preparation of schizophrenia drug Asenapine (Asenapine), can solve the problems of dangerous operation, high cost, high risk, etc., and achieve high yield, low production cost and simple operation Effect

Inactive Publication Date: 2013-08-21
甘肃皓天科技股份有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Both of these two reaction systems need to use anhydrous system, the reaction conditions are relatively harsh, and the operation is relatively dangerous.
Lithium aluminum tetrahydrogen and borane complexes are both flammable and explosive chemicals, which react violently with moist air or water, and are prone to combustion or explosion
A large amount of expensive lithium aluminum tetrahydrogen or borane is used in industry, which is dangerous and costly

Method used

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  • Preparation method of asenapine
  • Preparation method of asenapine
  • Preparation method of asenapine

Examples

Experimental program
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Effect test

Embodiment 1

[0011] Embodiment one : In the synthetic route shown in formula 2, wherein compound I is used as a raw material, the preparation of compound III: add 30 g of compound I to a 500 mL three-necked flask, dissolve it with 300 mL of toluene, and add 70% red Aluminum solution 144g. The reaction mixture was heated to 40°C to 50°C under constant stirring for 3 hours. Under cooling in an ice-water bath, add 100 mL of methanol dropwise to quench the reaction, add 100 mL of water and 200 mL of 10% sodium hydroxide solution, and stir for a while. The organic phase was separated, and the aqueous phase was extracted with 100 mL of dichloromethane. The organic phases were combined, dried, and concentrated under reduced pressure to recover the solvent to obtain 26 g of compound III with a yield of 71%.

Embodiment 2

[0012] Embodiment two : In the synthetic route shown in formula three, wherein compound II is used as a raw material, 30 g of compound I is added in a 500 mL three-necked flask, dissolved with 300 mL of toluene, and 144 g of 70% red aluminum solution is added dropwise at room temperature. The reaction mixture was heated to 40°C to 50°C under constant stirring for 3 hours. Under cooling in an ice-water bath, add 100 mL of methanol dropwise to quench the reaction, add 100 mL of water and 200 mL of 10% sodium hydroxide solution, and stir for a while. The organic phase was separated, and the aqueous phase was extracted with 100 mL of dichloromethane. The organic phases were combined, dried, and concentrated under reduced pressure to recover the solvent to obtain 25.5 g of compound III with a yield of 69%.

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Abstract

The invention discloses a preparation method of asenapine. According to the preparation method, the asenapine (III) is prepared from a compound I with formula 1 or a compound II with formula 2 under a vitride solution reduction condition. The method is high in yield and low in production cost due to the fact that vitride is much cheaper than borane; and moreover, vitride is safer and simpler to operate compared with the reagent used in the prior art, so that the asenapine is applicable to in-scale production.

Description

Technical field [0001] The present invention involves a preparation method for organic compounds, which is precisely as a preparation method that can be used as a schizophrenia. Background technique [0002] Asenapine, named Saphris, was developed by Organon Biosciences, produced by Schering Plough.On August 14, 2009, the FDA approved the drug for adult schizophrenia, mania, or an emergency treatment of mixed seizures with type I two -way emotional disorders. [0003] Arina Ping's English chemical name is: Trans-5-chloro-2,3,3A, 12B-Tetrahydro-2-Methyl-Dibenz [2,3: 6,7] oxepino [4,5-c] Pyrrole; Chinese Chemical Name: Real-5-chlorine-2,3,3A, 12B-Tethel Hydrogen-2-methyl-1H-diexy [2,3: 6,7] oxygen and mixed-C] Pyrhhho; molecular formula: C17H16CLNO; relative molecular weight: 285.77; CAS registration number: 65576-45-6.Since the emergence of Arina Ping, many patents and literature at home and abroad have reported their preparation methods.However, most of them are based on compound...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/044
Inventor 薛吉军
Owner 甘肃皓天科技股份有限公司
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