Antagonists Chlorphenamine Maleate raw powder

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Chlorphenamine Maleate Usage and Synthesis.

The indications are used for cold and allergic diseases of skin and mucous membrane, and the functions are mainly used for urticaria, eczema, dermatitis, drug rash, pruritus, neurodermatitis, insect bite, solar dermatitis, atopic dermatitis, vasomotor rhinitis, drug and food allergies. In addition to the competitive blocking of histamine H1 receptor on the target cells of allergy reaction, through the antagonism of H1 receptor plays an anti-allergic role, but also has an anti-M choline receptor effect, so after taking the drug can appear dry mouth, constipation, sputum thickening, dry nasal mucosa and other symptoms.

Uses of Chlorphenamine Maleate.

Antihistamines. Similar to Cloromitone, bromphenyramide is also an antihistamine. Bromphenyramide is also produced in a similar way to cloromitone, except that the starting material is replaced by a bromobenzene compound. The antihistamine effect of the product is more than diphenhydramine and promethazine, the dosage is small, the side effect is light. It is used for urticaria, vasodilator rhinitis, cold, asthma, rhinitis, contact dermatitis, and allergy caused by drugs and food, insect bites and motion sickness.

Pharmacological action of Chlorphenamine Maleate.

Chlorpheniramine is an H1 receptor antagonist, and its chemical structure belongs to hydrocarbon amines. It can competitively block the histamine H1 receptor on the target cells of allergic reaction, so that histamine cannot bind to the H1 receptor, so as to inhibit the allergic reaction caused by it. But chlorpheniramine does not affect histamine metabolism, nor does it prevent histamine release in the body. Chlorpheniramine also has central inhibition and anticholinergic effects, so after taking the drug, drowsiness, dry mouth, constipation, sputum thickening and dry nasal mucosa. After a long period of clinical practice, it is believed that the antihistamine effect of chlorpheniramine is strong, the dosage is small, and the side effects are small. The antihistamine effect of chlorpheniramine was stronger than that of diphenhydramine and promethazine, but the central inhibitory effect was weaker and the anticholinergic effect was weaker. Due to slight side effects such as drowsiness, it is suitable for children and patients who need to work during the day. Chlorpheniramine can also reduce the secretion of trachea and gastric acid. Before the advent of a new generation of antihistamines, it is the most commonly used antihistamine in the clinic.

Product Method of Bulk Chlorphenamine Maleate.

It is obtained by the two-step condensation of 2-p-chlorobenzylpyridine. In a dry reaction pot, sodium ammonia and anhydrous toluene were added, heated to reflux, and 2-p-chlorobenzylpyridine and bromoacetaldehyde diethyl ethanol were simultaneously dropped. Gabi, reflux reaction for 8h. Let it cool and stand, take toluene solution, and extract the solid with toluene after dissolving with a small amount of water. The extraction solution was combined with toluene solution, washed to neutral, and toluene was recovered to obtain 3-p-chlorobenzene - (2-pyridyl) -propanal diethyl alcohol. Mix it with DMF and add it to the reaction pot, stir and add the mixture of formic acid and water. It is heated to 110-120℃ for 2h and 150-160℃ for 3h. The DMF was recovered by cooling and decompression, diluted by heating water, and adjusted to pH14 with lye. Then extract with toluene, wash the extract liquid with water to neutral, recover toluene after vacuum distillation, collect 150-190℃ fraction, chlordromitone.

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