A kind of preparation method of tafluprost crude drug

Abstract

The invention discloses a preparation method of a tafluprost raw material drug, which comprises the preparation and separation of a high-efficiency preparation liquid phase, and the beating of C6-C8 alkane; the preparation method of the invention is stable in process and strong in operability, and can obtain other The total purity of the fluprostin is greater than 99.5%, wherein the impurity content of the trans isomer is less than 0.1%, and the content of other simple impurities is less than 0.1%.

Description

technical field

[0001] The invention belongs to the field of pharmacy, and in particular relates to a method for preparing tafluprost by efficiently preparing a liquid phase. Background technique

[0002] Tafluprost (Tafluprost) is a new type of prostaglandin analog developed and produced by Japan Santen Co., Ltd. It is mainly used for the treatment of open-angle glaucoma or ocular hypertension in patients with elevated intraocular pressure. The main mechanism of lowering intraocular pressure is to promote the outflow of aqueous humor through the uveal sclera to reduce intraocular pressure. The 15th hydroxyl group in the traditional prostaglandin analog structure is an essential functional group for prostaglandin receptor agonists to exert physiological activity. Tafluprost replaces this functional group with 2 F atoms. As an isopropyl ester, it can be Corneal esterase rapidly hydrolyzes to the free acid form, the active form of the drug. The affinity of tafluprost for the...

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