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US 12,497,374 B2Granted
Processes and intermediates for the preparations of benzoprostacyclin analogues and benzoprostacyclin analogues prepared therefrom
AssigneeChirogate International Inc.
InventorsChun-Yu Lin, Tzyh-Mann Wei, Shih-Yi Wei
Life of this patent
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Abstract
A racemic or optically enriched compound of Formula 1: wherein P is H or a protective group for hydroxyl groups; and X is Cl, Br, I, or —CH2CH2CH2COOR1, wherein R1 is C1-7-alkyl or C7-11-aralkyl.
Claims13
A racemic or optically enriched compound of Formula 1:
- wherein P is H or a protective group for hydroxyl groups;
- and X is Cl, Br, I, or —CH2CH2CH2COOR1, wherein R1 is C1-7-alkyl or C7-11-aralkyl.
A process for preparing a compound having the formula (R)-1″, wherein the compound is enriched in (R)-enantiomer and has an optical purity of at least 95% enantiomeric excess (e.e.),
- and
- wherein X is Cl, Br, or I, the process comprising the steps of:
- (1) enantioselectively (R)-esterifying a compound of Formula 1″:
- with an acyl donor of Formula D:
- wherein R4 and R5 are independently H or C1-6 alkyl, and a first lipase, to form a mixture of(S)-alcohol and (R)-ester;
- (2) optionally removing the(S)-alcohol;
- and
- (3) deacylating the (R)-ester.
5 more elements
Dependencies are inferred from the claim text.