1180843-77-9Relevant articles and documents
Preparation method of asenapine intermediate
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Paragraph 0027; 0035-0037; 0038; 0041, (2021/08/21)
The invention discloses a preparation method of an asenapine intermediate and belongs to the technical field of synthesis of asenapine intermediates. In the ASP07 preparation process, iodine is added for an initiation reaction, the reaction temperature is controlled to be 40 DEG C or below, inorganic acid is used for neutralization after the reaction is finished, hydrochloric acid and sulfuric acid are preferentially selected, inorganic base is used for a ring-opening reaction in the ASP08 preparation process, potassium hydroxide and sodium hydroxide are preferentially selected, the reaction temperature is 80-90 DEG C, and in the process of preparing the asenapine intermediate, ethanol and methanol are used as refining solvents, so that a high-purity product can be obtained. The asenapine intermediate is mainly applied to atypical antipsychotic drugs.
PROCESS FOR THE PREPARATION OF ASENAPINE MALEATE
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Paragraph 0054, (2015/04/28)
The present invention provides a process for the preparation of asenapine maleate of Formula (I), comprising: intra-molecular cyclization of the intermediate of Formula (II) to obtain the intermediate of Formula (III) using aluminium halide.
PROCESS FOR THE PREPARATION OF ASENAPINE INTERMEDIATE
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Page/Page column 8; 9, (2013/06/27)
The present invention provides a process for the preparation of the asenapine intermediate of Formula (III) using a magnesium-methanol-acetic acid mixture.