Method for producing itraconazole bulk drug
A technology of itraconazole and raw materials, applied in the field of production of itraconazole raw materials, can solve the problems of cumbersome procedures, long operation time, high energy consumption, etc., and achieve the reduction of the number of operators, the improvement of product yield, and the production The effect of labor intensity reduction
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Embodiment 1
[0020] This method is implemented in the raw material drug workshop of a certain pharmaceutical factory, with an annual output of 2 tons of itraconazole.
[0021] The production process of itraconazole bulk drug includes the preparation of nitro, amine, ring-closing, alkyl, hydroxyl, triazole and mesylate.
[0022] The preparation of itraconazole mainly includes two parts of main chain and side chain. The main chain is prepared as follows: the nitro compound is used as a starting material, and the fine nitro compound is obtained by dissolving with dioxane, crystallizing, filtering and drying. Under the catalysis of palladium carbon catalyst, in THF solvent, the nitro group in the nitro compound is reduced by hydrogen to carry out hydrogenation reaction, and then the amine compound is obtained through filtration, distillation, drying, etc. Under the catalysis of p-toluenesulfonic acid and sodium methoxide, in anhydrous ethanol solvent, amines react with methyl carbazate and tr...
Embodiment 2
[0035] According to the conditions and steps described in Example 1, the reaction temperature control system of the present invention is applied to the nitro substance preparation section, and the heat exchange medium is a mixture of 40% ethylene glycol and water. The three step temperatures of the same heat exchange medium are 160°C, 30°C, and -10°C.
[0036] Got the following data:
[0037] Product yield of itraconazole: 95%;
[0038] Public works consumption: the electricity used is equivalent to the production cost of 11,000 yuan / ton;
[0039]Reactor life: Slight abrasion begins to appear after 4-5 years of normal operation;
[0040] Section operator setting: intermittent operation, the number of operators on duty is 1;
[0041] Batch production auxiliary time: 10min.
Embodiment 3
[0043] According to the conditions and steps described in Example 1, the reaction temperature control system of the present invention is applied to the ring-closing compound preparation section, and the heat exchange medium is a mixture of 40% ethylene glycol and water. The three step temperatures of the same heat exchange medium are 130°C, 100°C, and -40°C.
[0044] Got the following data:
[0045] Product yield of itraconazole: 96%;
[0046] Public works consumption: the electricity used is equivalent to the production cost of 15,000 yuan / ton;
[0047] Reactor life: Slight abrasion begins to appear after 4-5 years of normal operation;
[0048] Section operator setting: intermittent operation, the number of operators on duty is 1;
[0049] Batch production auxiliary time: 10min.
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