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Method for synthesizing Blonanserin
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A synthetic method, the technology of blonanserin, applied in the direction of organic chemistry, can solve the problems of many side reactions, high pollution, strong irritation of chlorinated reagents, etc., and achieve simple and easy to control operation, low reaction temperature, and product purity Good results
Active Publication Date: 2013-01-23
HEBEI GUOLONG PHARMA CO LTD
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The main defects of these methods are: (1) the chlorinated reagent is highly irritating and highly polluting; (2) the chlorination reaction time of phosphorus oxychloride is long and the side reactions are many; (3) the selectivity of the intermediate B condensation reaction is poor
Intermediate B contains two aromatic molecular structures of chloropyridine and fluorobenzene, and fluorine and chlorine are atoms of the same family. N - During the reaction of ethylpiperazine, fluorine may also participate in the condensation reaction to produce impurity A (see the reaction formula below), which is formed in the last step of blonanserin and is difficult to remove, which affects the preparation of high-purity blonanserin
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[0034] Under stirring, dissolve 2.71g (10.0 mmol) of intermediate I in 40 mL of chloroform, add 1.93 g (10.2 mmol) of p-toluenesulfonyl chloride in 5 mL of chloroform, drop in 1.4 mL of pyridine, and stir at 40 °C Reaction, TLC monitors the completion of the reaction, pours the reactant into 100mL of water with stirring, adjusts the pH to neutral, adds methyl tert-butyl ether for extraction, separates the liquid, washes the extract with water, and removes the extract by rotary evaporation to obtain intermediate II-1 White solid, the crude product was recrystallized to obtain 3.18g of intermediate II-1, yield 75.3%, m.p.: 117~118 ℃.
[0041] According to the method of Example 1, the number of moles of p-toluenesulfonyl chloride was adjusted to be twice that of the reactant intermediate I, and the yield of intermediate II-1 was 83.5%.
[0043] According to the method of embodiment 1, the molar number of p-toluenesulfonyl chloride is adjusted to be 5 times, 10 times, 20 times of reactant intermediate I, and the yield of intermediate II-1 is all lower than 75%. Dealing with large losses.
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Abstract
The invention discloses a method for synthesizing Blonanserin, wherein the method comprises the following steps of taking 4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridin-2(1H)-one (which is named as an intermediate I) as an initial raw material, enabling the initial raw material to react with a substituted sulfonylchloride to obtain 4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridin-2-substituted sulphonate (which is named as an intermediate II-(1-n)), condensing the intermediate II-(1-n) with N-ethyl piperazine to obtain the Blonanserin, refining the obtained Blonanserin to obtain the Blonanserin with purity of 99.8%. The method provided by the invention prepares the Blonanserin raw material that has high purity and accords with the medicinal use by using a sulfonylation process; the method prepared by the invention has the advantages of high reaction selectivity, high product purity, low solventtoxicity, simple operation and easiness in control; the method provided by the invention is suitable for industrial production.
Description
technical field [0001] The invention relates to a method for synthesizing blonanserin, which belongs to the technical field of chemical medicine preparation. technical background [0002] Blonanserin (English name: Blonanserin) chemical name is 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10- Hexahydroaromatic [b]pyridine is a new generation of atypical anti-schizophreniadrug, which has a dopamine D2 receptor blocking effect comparable to that of haloperidol, and also has a strong blocking effect on 5-HT2A. The selectivity to the two receptors is stronger than other antipsychotic drugs, the safety and tolerance are obviously better than traditional antipsychotic drugs, and the side effects are small. [0003] [0004] The CAS number of blonanserin is 132810-10-7, and its molecular structure is as follows: [0005] At present, the disclosed synthetic method of blonanserin is mainly through the combination of halogenated pyridone and N - Prepared by condensati...
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