85650-55-1

Upstream product

• 110-16-7 maleic acid 
• 65621-78-5 asenapine 
• 1035404-17-1 ethyl N-[2-[2-(4-chlorophenoxy)phenyl]acetyl]-N-methylglycinate 
• 912356-09-3 cis-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one 
• 912356-09-3 trans-11-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one 
• 934996-79-9 5-chloro-2-methyl-2,3-dihydro-1H-dibenzo[2,3:6,7]oxepino [4,5-c]pyrrole-1-one 
• 25563-04-6 o-(p-chlorophenoxy)phenylacetic acid 
• 106-48-9 4-chloro-phenol 
• 2444-36-2 2'-chloro-benzeneacetic acid 
• 65621-78-5 asenapine 
• 6915-18-0 2-butenedioic acid 
• 934996-80-2 5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole-1-one 
• 1180843-77-9 trans-11-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz(2,3:6,7)oxepino(4,5-c)pyrrol-1-one 
• 912356-09-3 trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz(2,3:6,7)oxepino(4,5-c)pyrrol-1-one 

Downstream Products

• 65621-78-5 asenapine 
• 65621-78-5 asenapine 

Relevant academic research and scientific papers

Method for preparing the maleic acid Arab League fills evenly that

The invention discloses a preparation method of high-purity asenapine maleate. The preparation method comprises the following steps: by taking an asenapine free alkali crude product and a asenapine maleate crude product as an initial raw material, reacting the asenapine free alkali crude product with an organic acid to generate salt or carrying out alkalifying dissociation on the asenapine maleate crude product to asenapine free alkali to be reacted with the organic acid to generate salt so as to obtain asenapine para-benzyl benzyl; crystallizing, filtering and carrying out alkalifying dissociation to obtain asenapine free alkali; then reacting the product obtained from the former step with maleic acid to obtain asenapine maleate; and crystallizing and filtering. The preparation method of high purity asenapine maleate is novel in process route, mild in process condition and simple to operate, and an acceptable product with the purity greater than or equal to 99% can be obtained by just one time without repeatedly recrystallizing operations. Meanwhile, the preparation method further improves the reaction yield, lowers the production cost, is suitable for being applied to industrial production on a large scale, and has good practical value and social and economic benefits.

A method for the preparation of asenapine

The invention relates to a preparation method of a psychotropic medicine asenapine. The method comprises a step that asenapine is prepared through a reaction of a raw material trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-monobenzo[2,3:6,7]oxepino[4,5-C]pyrrole-1-one or trans-11-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenzo[2,3:6,7]oxepino[4,5-C]pyrrole-1-one under the action of a reducing agent sodium bisaluminumhydride or a composite reducing agent composed of sodium bisaluminumhydride and other regents. The method has the advantages of mild and controllable reaction technology, low production cost, good product yield, realization of the large scale application in the industrial production, and good enforcement values and social and economic benefits.

Compressed oral dosage form for asenapine maleate

The present invention relates to a compressed pharmaceutical dosage form intended for sublingual or buccal administration and capable of being rapidly disintegrated, the compressed pharmaceutical dosage form containing asenapine maleate in a microcrystalline monoclinic form. It further relates to a method of preparing the same and to a container comprising the dosage form.

PROCESS FOR PREPARING ASENAPINE AND SALTS OF INTERMEDIATES THEREOF

A process for preparing substantially pure trans-5-chloro-2-methyl-2,3,3a42b4etrahydro-lH-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole (Asenapine) of formula (I) is provided. The salts of intermediates useful for preparing Asenapine of formula (I) i.e. 5-nitro-2-methyl-2,3,3a,12b-tetrahydro-lH-dibenz [2,3:6,7] oxepino [4,5-c]pyrrole of formula (VIII) and 5-amino-2-methyl-2,3,3a,12b-tetrahydro-lH-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole of formula (DC) are also provided.

Amide activation by TMSCl: Reduction of amides to amines by LiAlH 4 under mild conditions

An expeditious and practical method for the reduction of amides to amines is reported. The method consists of activation of amides with TMSCl followed by reduction with LiAlH4. Various amides/lactams including hindered amides and secondary amides gave the corresponding amines in good to excellent yields. This novel protocol has a wide substrate scope and shows good functional group tolerance with high stereoretention.

IMPROVED PROCESS FOR THE PREPARATION OF ASENAPINE MALEATE

The present invention relates to a process for the preparation of Asenapine maleate with an avoiding column chromatography by use of DBN or DBA.

NOVEL PROCESS FOR THE PREPARATION OF ASENAPINE

The present invention relates to a novel process for the preparation of trans-5-chloro-2- methyl-2,3,3a,12b- tetrahydro-1H-dibenz [2,3:6,7] oxepino[4,5-c] pyrrole (Asenapine) of formula (I). It also relates to novel intermediates i.e. 2-[(E)-2-(2-bromophe

CRYSTAL FORM OF ASENAPINE MALEATE

The present invention relates to a form of Asenapine Maleate with XRPD peaks at about 5.5,12.5,19.0 and 25.3 and to methods for the preparation thereof. Furthermore the invention relates to a reproducible process for the preparation of pure monoclinic form of Asenapine Maleate in crystalline form and to pharmaceutical compositions comprising the pure monoclinic form of asenapine maleate.

A PROCESS FOR THE PREPARATION OF ASENAPINE AND NOVEL SALTS THEREOF

A process for preparation of asenapine of formula (1) or its acid addition salts; The said process comprises preparation of trans racemate of asenapine by reacting trans- 1 1-chloro-2,3,3a, 12b-tetrahydro-2-methyl-lH-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrol-l-one with mixture of aluminium chloride and lithium aluminium hydride in solvent followed by converting it into acid addition salt of asenapine followed by hydrolyzing the acid addition salt into trans racemate asenapine base and converting the asenapine base into acid addition salt. Asenapine sulphate of formula (Via) and asenapine maleate of formula (IVb) are also disclosed. The co-precipitate of acid addition salt of asenapine with a pharmaceutically acceptable excipient of formula (V); is also disclosed.

COMPRESSED ORAL DOSAGE FORM FOR ASENAPINE MALEATE

The present invention relates to a compressed pharmaceutical dosage form intended for sublingual or buccal administration and capable of being rapidly disintegrated, the compressed pharmaceutical dosage form containing asenapine maleate in a microcrystalline monoclinic form. It further relates to a method of preparing the same and to a container comprising the dosage form.