Adapalene Raw Materials Adapalene Powder

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Adapalene Raw Materials Powder Usage and Synthesis.

Adapalene belongs to the class of retinoic acid compounds, mainly binds to specific retinoic acid cell nuclear receptors; by normalising the differentiation of hair follicle epithelial cells, it reduces the formation of microcomedones, and it also relieves the inflammatory reaction of acne.

Uses and functions of Acyclovir Powder.

The retinoic acid analogue, adapalene, is a RARβ, and RARγ receptor agonist. Adapalene inhibits cell proliferation and induces apoptosis in colorectal cancer cells in vitro. Adapalene gel is an effective medication for the treatment of acne.

Pharmacological Effects of Adapalene Raw Powder.

Adapalene is a retinoid compound with proven anti-inflammatory properties in in vivo and in vitro models of inflammation, is chemically stable, and does not readily decompose in air and light.

It has the same mechanism of action as retinoic acid and binds to specific retinoic acid nuclear receptors, with the difference that adapalene does not bind to protein-bound cytoplasmic receptors. Adapalene has been shown to treat acne in dermal dosing trials in animal models established in mice, and has also been shown to have an effect on acne vulgaris and the differentiation process.

The mechanism of action is to reduce micro-acne formation by normalising the differentiation of hair cells on hair follicles.

In standard anti-inflammatory analyses in vivo and in vitro. Adapalene is more effective than retinoic acid in inhibiting chemotaxis of human polymorphonuclear leukocytes and inhibiting the metabolism of polymorphonuclear meningoar by inhibiting the conversion of arachidonic acid to inflammatory mediator mediators via lipid oxidation, thus alleviating inflammatory reactions mediated by cellular responses. It is indicated for the treatment of acne vulgaris with pimples, papules and pustules as the main manifestations. It can also be used to treat acne on the face, chest and back.

Production method of Adapalene.

(1) Under nitrogen atmosphere, 356 g (1.0 mol) of 2-methoxycarbonyl-6-naphthol p-toluenesulfonate, 332 g (0.65 mol) of bis(4-methoxy-3-adamantylphenyl) boronic acid, 533 g (2 mol) of potassium phosphate trihydrate, 6.5 g (0.01 mol) of bis(triphenylphosphine)nickel chloride and 2.2 g ( 0.01 mole) N-methyl-N'-butylimidazole ammonium salt of bromide and 1.0 L of toluene solvent were reacted at 120 °C with stirring until the end, and the reaction solution was cooled to room temperature.

(2) Wash the reaction solution obtained in step (1) with saturated brine, separate out the organic phase, dry Chemicalbook and then distillate at atmospheric pressure to recover the solvent, recrystallise the resulting solid with toluene, precipitate the solid after cooling, and filter, to obtain 6-[3-(1-adamantyl)-4-methoxyphenyl]-2- naphthalene carboxylic acid methyl ester.

(3) Dissolve 160g (4 moles) of sodium hydroxide with 0.5L of methanol, add it to methyl 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthalenecarboxylate obtained in step (2), and heat and reflux until the reaction of methyl 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthalenecarboxylate is complete.

(4) The organic solvent was removed by distillation under atmospheric pressure, the pH was adjusted to 1, and 367 g of adapalene was obtained by filtration.

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