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Base‐Promoted Isomerization of cis ‐Lactam to trans ‐Lactam of Asenapine and Optimization of Crystallization Process of Asenapine Maleate Salt: An Antipsychotic Drug
Author(s) -
Vinigiri Krishna,
Kammari Bal Raju,
Rao P Narasimha,
Kotu Girija Mangatayaru
Publication year - 2019
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201900658
Subject(s) - crystallization , lactam , asenapine , chemistry , isomerization , combinatorial chemistry , organic chemistry , antipsychotic , catalysis , schizophrenia (object oriented programming) , computer science , programming language
Abstract We have described the development of commercially scalable synthetic process for Asenapine, an antipsychotic drug. This involved the isomerization of cis ‐lactam compound 5 to required trans ‐lactam compound 6 and followed by isolation without chromatographic technique. The isolation process was executed up to 10 kg batch scale and achieved with good yield and high purity of trans ‐lactam compound 6 . We have also developed a crystallization process to obtain the stable and pure microcrystalline monoclinic form of asenapine maleate even after micronization with desirable particle size, which was previously unpredictable from the reported crystallization process.