4.4 Article

Efficient synthesis of (-)-(R)- and (+)-(S)-rolipram

Journal

TETRAHEDRON LETTERS
Volume 58, Issue 46, Pages 4333-4335

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2017.09.080

Keywords

Rolipram; Michael addition; Henry condensation; gamma-Aminobutyric acid; Antidepressant

Funding

  1. Department of Science and Technology (DST-SERB), New Delhi [EMR/2016/003649]
  2. UGC, New Delhi

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A novel, efficient and protecting group free enantioselective synthetic approach of (-)-(R)-1 and (+)-(S)-rolipram 2 is described employing the organocatalyzed asymmetric Michael addition, Henry condensation, Wittig olefination and reductive lactamization reactions as key steps. (C) 2017 Elsevier Ltd. All rights reserved.

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