| Beraprost sodium is a prostacyclin derivatives. In parallel with a benzene ringon prostacyclin secondary five-membered ring, It can increase the stability of themolecule. Beraprost sodium is the first prostacyclin analogue drug which can beoral and stable.Its half-life in the body for35-40min. Clinically used to treat chronic arterialocclusion. Now it is proved that beraprost sodium have a significant effect totreat pulmonary hypertension. It has received the approval of the Japanesepharmacopoeia to treat pulmonary hypertension. and FDA approved its entry ofphase II clinical trial. The excessive demand for beraprost sodium because of itseffective treatment for chronic arterial occlusion and other diseases. There is onlyone joint venture for the production in china. So we developed a simple andefficient method to synthesize beraprost sodium. It has a very important practicalsignificance and market value.We provide a new method for the synthesis of beraprost sodium. We firstly usemore cheaper cyclopentadiene dimer as the starting material. By one-pot reaction toget3,5-cis-bis(2,4,6-tribromophenoxy)-1-cyclopentene. It is easy to industrialproduction by the above two reasons.We provide a new synthetic method of compound (Ⅳ) to compound (Ⅵ).Specifically relate to compounds (Ⅵ)4-(2,3,3a,8b-tetrahydro-1-hydroxy-2-aceticmethyl-1H-cyclopenta[b]benzofuranyl)butanoate. The compound (Ⅳ) is rawmaterial. We get the purity compound (Ⅵ) through two steps reaction. In thismethod. We guarantee a high yield and avoid the palladium-carbon activitydecreased.We provide an inexpensive method for the preparation of compound A. Tocheap γ-butyrolactone as raw material, compound A is synthesized through ring- opening reaction, oxidation reaction. Reducing the cost of compound A. Byoptimizing the three points, we can synthesize qualified beraprost sodium throughthe eight-steps reaction. And using cheaper raw material. It is very meaningful forthe patients who use the economic beraprost sodium. |
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