88277-10-5

Upstream product

• 84598-98-1 cis-1,4-bis(2,4,6-tribromophenoxy)cyclopent-2-ene 
• 3784-04-1 potassium 2,4,6-tribromophenoxide 
• 124-38-9 carbon dioxide 
• 84599-02-0 3a,8b-cis-dihydro-3H-5,7-dibromocyclopentabenzofuran 

Relevant academic research and scientific papers

Preparative resolution of a key intermediate for the synthesis of optically active m-phenylene PGI2 derivatives

A key intermediate for the synthesis of optically active m-phenylene PGI2 derivatives was efficiently resolved on a preparative scale by diastereomeric salt formation method using (+)-cis-N-benzyl-2- (hydroxymethyl)cyclohexylamine ((+)-cis-amine) as a resolving agent.

Synthesis method of beraprost sodium intermediate

The invention relates to a synthesis method of a Beraprost sodium intermediate (III). Cyclopentene and N-bromo-succinimide (NBS) carry out free radical reaction to obtain dibromocyclopentene; and dibromocyclopentene reacts with 2,4,6-tribromophenol to directly generate 3,5-bis(2,4,6-tribromophenoxyl) cyclopentene (compound I) through a one-pot method. Then through Grignard reactions, a compound (I) and a compound (II) are obtained. N-bromo-succinimide and a commercial product namely cyclopentene are taken as the raw materials to synthesize dibromocyclopentene, 170 DEG C cracking and ultralow temperature reactions (-40 to -30 DEG C) are avoided, the using of bromine is also avoided, the reaction conditions are milder, and the synthesis method is more environmentally friendly and is convenient for industrial production.

Synthesis of (+)-5,6,7-trinor-4,8-inter-m-phenylene PGI2

The titled compound, which is a stable and potent analog of prostacyclin, was synthesized from readily available 1,4-dibromocyclopentene via cyclopenta[b]benzofuran carboxylic acid 5.