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Preparation method of olanzapine

A compound and water-absorbing agent technology, applied in organic chemistry and other directions, can solve problems such as affecting the quality of olanzapine medicinal products, reducing product purity, and difficult to remove impurities

Active Publication Date: 2013-02-27
连云港恒运药业有限公司
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Problems solved by technology

[0015] 2) In the step of preparing olanzapine from desmethyl olanzapine of formula (III), another secondary nitrogen in desmethyl olanzapine will be methylated to obtain the compound of formula (VII) or be acylated , and the impurity is not easy to remove, which reduces the purity of the product and affects the quality of olanzapine as a pharmaceutical product

Method used

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  • Preparation method of olanzapine

Examples

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Embodiment 1

[0041] 1, the preparation of 2-amino-5 methyl-3-thiophenecarbonitrile

[0042] Sulfur (21.8g, 0.68mol), propionaldehyde (47.3g, 0.81mol) and DMF (135ml) were added to the reaction flask, and triethylamine (57.6mol, 0.41mol) was added dropwise at 5-10°C for about 30 minutes After the addition is completed, react at 18-20°C for 1 hour, add a mixture of malononitrile (45g, 0.68mol) and DMF (90ml) dropwise, and add it for about 1 hour, then continue to react at 15-20°C for 1 hour, and the reaction The solution was washed into ice water to produce a yellow precipitate, which was allowed to stand, filtered, washed with water, and dried under pressure to obtain a yellow solid (70 g), yield 74.6%, mp 99-100°C.

[0043]

[0044] 2. Preparation of 2-(2-nitrophenylamine)-5 methyl-3-thiophenecarbonitrile

[0045] In a solution of sodium hydride (14.4g, 50%, 0.3mol) and THF (50ml), 2-fluoronitrobenzene (28.2g, 0.2mol) and 2-amino-5methyl-3-thienylbenzene were added dropwise The mixtur...

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Abstract

The invention relates to a preparation method of olanzapine shown in the formula (I). Through water absorbent utilization, reagent concentration adjustment and selection of an appropriate crystallization mode, the preparation method realizes impurity reduction and yield improvement.

Description

technical field [0001] The present invention relates to a preparation method of olanzapine represented by formula (I), especially a preparation method for reducing impurities and increasing yield by adding a water-absorbing agent, adjusting reagent concentration and selecting a suitable crystallization method. Background technique [0002] There are currently many antipsychotics, among which thienobenzodiazepines are one class, and this class of compounds is disclosed in British Patent No. 1533235, which has the following general formula. [0003] [0004] Among this class of compounds, one of them has been found: 2-Methyl-10-(4-methyl-piperazinyl)-4H-thieno[2,3-b][1,5]benzazepine Zhuo (formula I), or its acid addition salt has obvious advantages, [0005] [0006] A separate patent was applied for this compound (US Patent No. 5,229,382). The common name of this compound is Olanzapine. In addition, olanzapine has a Chinese patent (ZL91103346.7) on a preparation metho...

Claims

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Application Information

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IPC IPC(8): C07D495/04
Inventor 袁阜平范建国
Owner 连云港恒运药业有限公司
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