IP Library › Granted Patent US 8,658,837
Granted Patent B2
US 8,658,837 · App. 13/954,191 · Granted Feb 25, 2014

Intermediates for the synthesis of benzindene prostaglandins and preparations thereof

Inventors: Shih-Yi Wei (Yangmei, TW); Min-Kuan Hsu (Yangmei, TW); Ming-Kun Hsu (Yangmei, TW)
Assignee: Chirogate International Inc.
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Quick Facts
Patent No.
US 8,658,837
App. No.
13/954,191
Granted
Feb 25, 2014
Kind
B2
Abstract

Novel processes for preparing optically active cyclopentanones 1 which are useful for the preparation of benzindene Prostaglandins and novel cyclopentanones are provided. The invention also provides novel processes of preparing benzindene Prostaglandins and novel intermediates for benzindene Prostaglandins.

Claims (13)

1. A process for preparing the compound of Formula 8d

comprising the steps of:

(1) esterifying the compound of Formula 6d

wherein P 2 and P 3 are protecting groups for the hydroxyl groups, to form an ester compound of Formula 10d

wherein M is a lower alkyl, or an unsubstituted or substituted phenyl;

(2) removing the P 2 and P 3 groups to form a compound of Formula 11d

(3) hydrogenating the double bond in the ω-side chain of the compound of Formula 11d and then deacylating the hydrogenated compound; or deacylating the compound of Formula 11d and then hydrogenating the double bond in the ω-side chain of the deacylated compound to form a compound of Formula 8d.

2. The process according to claim 1 , wherein M is phenyl or 4-phenylphenyl.

3. A compound of Formula 1e

wherein P 1 is an unsubstituted or substituted benzyl; is single bond or double bond; R 2 is a single bond or a C 1-4 -alkylene or —CH 2 O—; R 3 is a C 1-7 -alkyl or an aryl or an aralkyl group, each of which is unsubstituted or substituted by a C 1-4 -alkyl, a halogen, or a trihalomethyl; P 2 ′ and P 3 ′ are respectively P 2 and P 3 as defined in claim 1 as protecting groups for the hydroxy group or are independently H.

4. A compound of Formula 8D-1

5. A compound of Formula 11-1

wherein M is methyl, phenyl or 4-phenylphenyl; and is a single or double bond.

Continuity (2)
Division 13216378 · Aug 24, 2011
Related Publication 20130317245A1 · Nov 28, 2013