- PROCESS FOR PREPARATION OF MOLINDONE
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The present invention provides process for preparation of molindone (I) comprising: a) reacting compound with cyclohexane-1,3-dione to form 2-(2-oxopentan-3-yl)cyclohexane-1,3-dione wherein X is Cl, Br or I, b) cyclizing 2-(2-oxopentan-3-yl)cyclohexane-1,
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- Improved synthesizing method of molindone
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The invention relates to the field of medicine synthesizing, and particularly relates to an improved synthesizing method of molindone. The improved synthesizing method of the molindone comprises the following steps of (1) under the condition of existence of an alcohol solvent and an ore acid catalyst, enabling 2-methyl-3-ethyl-4,5,6,7-tetrehydro indole-4-ketone, morpholine hydrochloride and paraformaldehyde to perform aminomethylation reaction at the temperature of 50 to 55 DEG C under the condition of refluxing reaction, so as to generate molindone hydrochloride; (2) separating out the unreacted raw material, namely 2-methyl-3-ethyl-4,5,6,7-tetrehydro indole ketone, and alkalifying a mother liquid, so as to directly obtain the molindone. The improved synthesizing method has the advantages that the usage amount of solvent in the Mannich reaction is reduced by times, the aminomethylation reaction time is greatly shortened, the subsequent impurity removal separation process is simplified, the yield rate is high, the cost is low, the production environment is obviously improved, the treatment cost of three wastes is low, and the comprehensive advantages are obvious.
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Paragraph 0082-0085
(2017/09/01)
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