Patent classifications
C
CHEMISTRY; METALLURGY
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C07
ORGANIC CHEMISTRY
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C07C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
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405/00
Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins; ; Analogues or derivatives thereof
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C07C405/0008
Analogues having the carboxyl group in the side-chains replaced by other functional groups
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C07C405/0041
containing nitrogen
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C07C405/0041

Processes and intermediates for the preparations of isomer free prostaglandins
09540311 · 2017-01-10 · ·

Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: ##STR00001##
wherein ##STR00002##
R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.

INDUSTRIAL PROCESS FOR THE PREPARATION OF HEXANOIC ACID, 6-(NITROOXY)-, (1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(ETHYLAMINO)-7-OXO-2-HEPTEN-1-YL]-3,5-DIHYDROXYCYCLOPENTYL]-1-(2-PHENYLETHYL)-2-PROPEN-1-YL ESTER AND HIGH PURE PRODUCT
20250320182 · 2025-10-16 ·

The present invention relates to a process for preparing hexanoic acid, 6-(nitrooxy)-, (1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(ethylamino)-7-oxo-2-hepten-1-yl]-3,5-dihydroxycyclopentyl]-1-(2-phenylethyl)-2-propen-1-yl ester

##STR00001##

In accordance with the present invention, a pharmaceutical grade Compound (I) can be efficiently prepared by a one-pot reactions preparation step that includes the esterification of the 15-OH bimatoprost by coupling bimatoprost phenyl-boronate with 6-(nitrooxy) hexanoic acid and the removal of the boronate ester protecting group, followed by an efficient purification step.

The invention refers also to high purity Compound (I) substantially free of the impurity 15-(6-chlorohexanoyl) ester of bimatoprost and to ophthalmic pharmaceutical formulations containing the high purity compound.