Pharmaceutical Adapalene Raw Materials Powder CAS 106685-40-9 API Factory Supply

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Adapalene Powder Usage and Synthesis.

Adapalene Powder is mainly used to improve inflammatory skin lesions, modulate the differentiation of epithelial cells in hair follicles and sebaceous glands, and in the treatment of acne.

Adapalene Raw Materials is a retinoid analogue with proven anti-inflammatory properties in in vivo and in vitro models of inflammation, a stable chemical structure, and is not readily broken down by exposure to air and light.

Adapalene is a retinoic acid analogue and a RARβ and RARγ agonist. The retinoic acid analogue, adapalene, is a RARβ, and RARγ receptor agonist.Adapalene CAS 106685-40-9 inhibits cell proliferation and induces apoptosis in colorectal cancer cells in vitro. 

Adapalene Gel is an effective medication for the treatment of acne.

Uses and functions of Adapalene Powder.

Adapalene, as a 3rd generation retinoid, has strong anti-inflammatory properties in addition to having stronger effects than retinoids such as all-trans retinoic acid in regulating epidermal cell differentiation, inhibiting keratinocyte proliferation and keratinisation at the mouth of the hair follicle, inhibiting sebaceous gland cell proliferation, and dissolving keratosis pilaris and acne. Because of its unique stability, it has significantly improved its efficacy and tolerability compared to other retinoids.

Pharmacological Effects of Adapalene 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 Powder.

• (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) The reaction solution obtained in step (1) was washed with saturated brine, the organic phase was separated, dried and distilled at atmospheric pressure to recover the solvent, the resulting solid was recrystallised from toluene, the solid was precipitated after cooling and filtered 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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