85650-55-1Relevant articles and documents
Method for preparing the maleic acid Arab League fills evenly that
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Paragraph 0024, (2017/03/08)
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.
Amide activation by TMSCl: Reduction of amides to amines by LiAlH 4 under mild conditions
Ravinder,Rajeswar Reddy,Panasa Reddy,Bandichhor, Rakeshwar
supporting information, p. 4908 - 4913 (2013/08/28)
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
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, (2013/03/26)
The present invention relates to a process for the preparation of Asenapine maleate with an avoiding column chromatography by use of DBN or DBA.