Synthesis of iloperidone / 军事医学
Military Medical Sciences
;
(12): 271-275, 2015.
Article
in Chinese
| WPRIM
| ID: wpr-464107
ABSTRACT
Objective To optimize the synthesis process of iloperidone 1 for industrial production.Methods Piperi-dine-4-carboxylic acid, acetic acid and acetic anhydride were used as starting materials to generate 2 via amidation, Friedel-Crafts acylation, hydration, oximation, intramolecular cyclization and salification.Compound 2 was treated with 4-(3-chloropropoxy)-3-methoxyphenylethanone through condensation to afford iloperidone.The target compound 1 was prepared with an overall yield of 34.9%.Results and Conclusion Such factors as the ratio of the raw materials, the catalyst, reactive time were investigated and optimized to make the reaction conditions mild and easy to control with less side effects.The structure has been confirmed by IR, 1 H-NMR and MS.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Military Medical Sciences
Year:
2015
Type:
Article
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