An improved process for the preparation of Dolutegravir
AssigneeAurobindo Pharma Ltd
InventorsShankar Reddy Budidet, Nageshwar Dussa, Gowrisankar Rao Kaki, Srinivasa Rao Yatcherla, Jagan Mohan Reddy Sanapureddy, Subba Reddy Danda, Srinivasachary Katuroju, Sivakumaran Meenakshisunderam
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Abstract
The present invention provides (R)-3-Amino-1-butanol (D)-tartarate (IIb); process for its preparation and its conversion to Dolutegravir. The present invention also provides an improved process for the preparation of Dolutegravir (I) or pharmaceutically acceptable salts wherein compound (XVI) is reacted with an optically active acid addition salt of (R)-3-amino-1-butanol (IIa).
Claims16
(R)-3-Amino-1-butanol (D)-tartarate (Formula IIb).
(canceled)
A process for the preparation of (R)-3-amino-1-butanol (D)-tartrate salt (Formula IIb),
- which comprises, reacting (R,S)-3-amino-1-butanol (Formula XXV)
- with (D)-tartaric acid to produce (R)-3-amino-1-butanol (D)-tartrate salt (Formula IIb).
(canceled)
(canceled)
A process for the preparation of (R)-3-amino-1-butanol (Formula II) or optically active addition salt thereof,
- which comprises:
- (i) hydrogenating 4-hydroxy-2-butanone oxime (Formula XXIV),
- to produce (R,S)-3-amino-1-butanol (Formula XXV),
- (ii) treating the compound (XXV) with optically active carboxylic acid to produce diastereomeric salt of (R)-3-amino-1-butanol optically active acid (Formula IIa),
- wherein, OA refers optically active acid,
- (iii) optionally, converting the compound (IIa) to (R)-3-amino-1-butanol (Formula II).
(canceled)
(canceled)
15-42. (canceled)
A process for the preparation of Dolutegravir (Formula I), which uses (R)-3-Amino-1-butanol (D)-tartarate (Formula IIb) as a starting or intermediate material.
Dependencies are inferred from the claim text.