1355026-91-3

Upstream product

• 1365392-91-1 methyl {3-[(2,2,2-trifluoroethoxy)methyl]phenyl}acetate 
• 756-79-6 dimethyl methane phosphonate 
• 626-15-3 1,3-bis-(bromomethyl)benzene 

Downstream Products

• 1365391-90-7 ethyl 7-[(2R)-2-{(1E,3S)-3-hydroxy-4-[3-(2,2,2-trifluoroethoxymethyl)phenyl]-1-buten-1-yl}-5-oxo-1-pyrrolidinyl]heptanoate 
• 494221-69-1 7-((2R)-2-{(1E,3S)-3-hydroxy-4-[3-(2,2,2-trifluoroethoxymethyl)phenyl]-1-buten-1-yl}-5-oxo-1-pyrrolidinyl)heptanoic acid 
• 1365392-14-8 methyl 4-[(2-{(2R)-2-[(1E,3S)-3-hydroxy-4-{3-[(2,2,2-trifluoroethoxy)methyl]phenyl}-1-buten-1-yl]-5-oxo-1-pyrrolidinyl}ethyl)thio]butanoate 
• 494222-22-9 4-[(2-{(2R)-2-[(1E,3S)-3-hydroxy-4-(3-(2,2,2-trifluoroethoxymethyl)phenyl)but-1-enyl]-5-oxopyrrolidin-1-yl}ethyl)sulfanyl]butanoic acid 

Relevant academic research and scientific papers

Discovery of a novel EP2/EP4 dual agonist with high subtype-selectivity

A series of γ-lactam prostaglandin E1 analogs bearing a 16-phenyl moiety in the ω-chain and aryl moiety in the α-chain were synthesized and biologically evaluated. Among the tested compounds, γ-lactam PGE analog 3 designed as a structural hybrid of 1 and 2 was discovered as the most optimized EP2/EP4 dual agonist with excellent subtype-selectivity (Ki values: mEP2 = 9.3 nM, mEP4 = 0.41 nM). A structure-activity relationship study is presented.

Discovery of orally available 8-aza-5-thiaProstaglandin E1 analogs as highly selective EP4 agonists

Analogs 8-aza-16-aryl prostaglandin E1 (PGE1) and 8-aza-5-thia-16-arylPGE1 were synthesized and evaluated with respect to their subtype receptor affinity and EP4 agonist activity for the purposes of identifying sub-type- selective EP