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Triflumizole original drug, and preparation method thereof

A technology of fluconazole and the original drug, which is applied in the field of fluconazole original drug and its preparation, can solve the problems that the flucloxanil original drug is not easy to operate, the intermediate is not pure, and the environment is easy to pollute, and it is difficult to handle, intermediate Purify the body and reduce environmental pollution

Active Publication Date: 2019-08-09
JIANGSU HEBEN BIOCHEM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a kind of fluconazole technical substance and preparation method thereof, solve the problems of the fluclofenazole technical substance not easy to operate, easy to pollute the environment, impure intermediates, low yield etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] A kind of flufenazole former drug

[0029] The raw materials and parts by weight for the preparation of the technical flufenazole are: 370kg of chloroacetic acid, 5kg of diazabicyclo, 110kg of n-propanol, 800kg of sodium n-propoxide, 650kg of ether, 30kg of concentrated sulfuric acid, 20kg of isoamyl nitrite, Toluene 400kg, 2-trifluoromethyl-4-chloroaniline 600kg, imidazole 410kg, cyclohexane 1000kg, triphosgene 450kg, chloroform 1400kg, triethylamine 180kg.

[0030] The preparation method of the former medicine of fluconazole, the steps are as follows:

[0031] Step S1, stirring the parts by weight of chloroacetic acid, diazabicyclo and half of the parts by weight of n-propanol for 30 minutes to obtain material A;

[0032] Step S2, put the weight portion of sodium n-propoxide and the remaining part of n-propanol into the reaction kettle and stir for 10 minutes, add material A at a temperature of 40°C to 50°C and keep it warm for 4 hours, raise the temperature to 100°C...

Embodiment 2

[0036] A kind of flufenazole former drug

[0037] The raw materials and parts by weight for preparing fluclopyridine are: 390kg of chloroacetic acid, 8kg of diazabicyclo, 115kg of n-propanol, 810kg of sodium n-propoxide, 690kg of ether, 40kg of concentrated sulfuric acid, 25kg of isoamyl nitrite, Toluene 420kg, 2-trifluoromethyl-4-chloroaniline 650kg, imidazole 430kg, cyclohexane 1100kg, triphosgene 460kg, chloroform 1500kg, triethylamine 190kg.

[0038] The preparation method of the former medicine of fluconazole, the steps are as follows:

[0039] Step S1, stirring the parts by weight of chloroacetic acid, diazabicyclo and half of the parts by weight of n-propanol for 40 minutes to obtain material A;

[0040]Step S2, put the weight portion of sodium n-propoxide and the rest of n-propanol into the reaction kettle and stir for 10 minutes, add material A at a temperature of 40°C to 50°C for 4.5 hours, raise the temperature to 110°C for distillation Recover n-propanol, then ad...

Embodiment 3

[0044] A kind of flufenazole former drug

[0045] The raw materials and parts by weight for the preparation of the technical flufenazole are: 400kg of chloroacetic acid, 10kg of diazabicyclo, 120kg of n-propanol, 820kg of sodium n-propoxide, 700kg of ether, 50kg of concentrated sulfuric acid, 30kg of isoamyl nitrite, Toluene 450kg, 2-trifluoromethyl-4-chloroaniline 700kg, imidazole 440kg, cyclohexane 1200kg, triphosgene 470kg, chloroform 1700kg, triethylamine 200kg.

[0046] The preparation method of the former medicine of fluconazole, the steps are as follows:

[0047] Step S1, stirring the parts by weight of chloroacetic acid, diazabicyclo and half of the parts by weight of n-propanol for 50 minutes to obtain material A;

[0048] Step S2, put the said weight portion of sodium n-propoxide and the remaining part of n-propanol into the reactor and stir for 10 minutes, add material A at a temperature of 40°C to 50°C and keep it warm for 5 hours, raise the temperature to 120°C f...

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Abstract

The invention provides a triflumizole original drug, and a preparation method thereof. The triflumizole original drug comprises, by weight, 370 parts to 400 parts of chloroacetic acid, 5 parts to 10 parts of diazabicyclo, 110 parts to 120 parts of n-propanol, 800 parts to 820 parts of sodium n-propoxide, 650 parts to 700 parts of diethyl ether, and 30 parts to 50 parts of concentrated sulfuric acid, 20 parts to 30 parts of isoamyl nitrite, 400 parts to 450 parts of toluene, 600 parts to 700 parts of 2-trifluoromethyl-4-chloroaniline, 410 parts to 440 parts of imidazole, 1000 parts to 1200 parts of cyclohexane, 450 parts to 470 parts of triphosgene, 1400 parts to 1700 parts of chloroform, and 180 parts to 200 parts of triethylamine. The total yield of the triflumizole original drug is higher than 85%, the original drug content is higher than 95%, the water content is less than 0.5, the drug effect is remarkable, and the effect is better.

Description

technical field [0001] The invention relates to the technical field of fluconazole, in particular to a technical field of fluconazole and a preparation method thereof. Background technique [0002] The pure fluconazole is a colorless crystal, and the original drug is a light yellow solid with a melting point of 63.5°C, slightly soluble in water, and easily soluble in organic solvents such as chloroform, acetone, xylene, and methanol. It is unstable in concentrated alkali and acid medium; its aqueous solution is easily degraded under sunlight. The acute oral LD50 of flufenazole to rats is 715mg / kg (male) and 695mg / kg (female); the acute percutaneous LD50 of rats and mice is more than 5000mg / kg. Irritation; no teratogenic, mutagenic, carcinogenic effects. The drug is a high-efficiency, low-toxicity, and low-residue systemic fungicide containing fluoroimidazole heterocycles. It has both protective and therapeutic effects. It is widely used in the prevention and treatment of p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/61
CPCC07D233/61
Inventor 陈华曾挺潘光飞
Owner JIANGSU HEBEN BIOCHEM
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