Thursday, August 23, 2012
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gram-scale synthesis of prostaglandins
A method for synthesizing
prostaglandins could help generate new compounds using fewer manufacturing
steps. Synthesis of prostaglandin analogs is complicated, and drugs such as Xalatan
latanoprost are still
manufactured via a 20-step process. A two-step reaction sequence from
inexpensive starting materials produced gram-scale quantities of a bicyclic enal
intermediate. A five-step reaction sequence converted the enal intermediate
to gram-scale quantities of prostaglandin F2a (PGF2a).
Ongoing work includes testing the biological activity of compound libraries
generated from the enal intermediate.
F receptor (PTGFR)
agonist from Pfizer
Inc., is marketed to decrease intraocular pressure in
At least 11 companies market prostaglandins or prostaglandin analogs to treat
cardiovascular, ophthalmic, genitourinary and gastrointestinal diseases.
Published online Aug. 23, 2012
Patented; available for
Coulthard, G. et al.
published online Aug. 15,
Contact: Varinder K. Aggarwal,
University of Bristol,
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