Continuous flow asymmetric synthesis of chiral active pharmaceutical ingredients and their advanced intermediates

SB Ötvös, CO Kappe - Green Chemistry, 2021 - pubs.rsc.org
Catalytic enantioselective transformations provide well-established and direct access to
stereogenic synthons that are broadly distributed among active pharmaceutical ingredients …

Recent developments in next generation (S)-proline-derived chiral organocatalysts

E Juaristi - Tetrahedron, 2021 - Elsevier
In the area of asymmetric organocatalysis, significant effort has been dedicated during the
last decade to improve the performance of emblematic catalysts such as proline, as well as …

Recent advances in continuous-flow organocatalysis for process intensification

C De Risi, O Bortolini, A Brandolese… - Reaction Chemistry & …, 2020 - pubs.rsc.org
Chemistry in continuous-flow continues to attract attention from the community of synthetic
organic chemists due to its now well-recognized benefits including, inter alia, quick reaction …

Telescoped continuous flow synthesis of optically active γ-nitrobutyric acids as key intermediates of baclofen, phenibut, and fluorophenibut

SB Ötvös, P Llanes, MA Pericàs, CO Kappe - Organic letters, 2020 - ACS Publications
The two-step flow asymmetric synthesis of chiral γ-nitrobutyric acids as key intermediates of
the GABA analogues baclofen, phenibut, and fluorophenibut is reported on a multigram …

Recent applications of mechanochemistry in enantioselective synthesis

CG Avila-Ortiz, M Pérez-Venegas, J Vargas-Caporali… - Tetrahedron …, 2019 - Elsevier
In recent years, sustainable organocatalysis has become a relevant target in asymmetric
organic synthesis. Among the most successful strategies to achieve “greener” …

Recent advances in continuous‐flow enantioselective catalysis

T Yu, Z Ding, W Nie, J Jiao, H Zhang… - … A European Journal, 2020 - Wiley Online Library
The increased demand for more efficient, safe, and green production in fine chemical and
pharmaceutical industry calls for the development of continuous‐flow manufacturing, and for …

Profiling the privileges of pyrrolidine-based catalysts in asymmetric synthesis: From polar to light-driven radical chemistry

A Vega-Penaloza, S Paria, M Bonchio… - ACS …, 2019 - ACS Publications
Asymmetric catalysis is a rapidly evolving field in synthetic chemistry. This is due to the
growing needs of stereoselective synthetic routes to access enantiopure natural products …

Multigram-scale flow synthesis of the chiral key intermediate of (−)-paroxetine enabled by solvent-free heterogeneous organocatalysis

SB Ötvös, MA Pericàs, CO Kappe - Chemical Science, 2019 - pubs.rsc.org
The catalytic enantioselective synthesis of the chiral key intermediate of the antidepressant
(−)-paroxetine is demonstrated as a continuous flow process on multi-gram scale. The …

Enantioselective Flow Synthesis of Rolipram Enabled by a Telescoped Asymmetric Conjugate Addition–Oxidative Aldehyde Esterification Sequence Using in Situ …

BS Nagy, P Llanes, MA Pericas, CO Kappe… - Organic …, 2022 - ACS Publications
A novel approach is reported for the enantioselective flow synthesis of rolipram comprising a
telescoped asymmetric conjugate addition–oxidative aldehyde esterification sequence …

Asymmetric Synthesis of Isoxazol-5-ones and Isoxazolidin-5-ones

A Macchia, A Eitzinger, JF Brière, M Waser… - Synthesis, 2021 - thieme-connect.com
Isoxazol-5-ones and isoxazolidin-5-ones represent two important classes of heterocycles,
with several applications as bioactive compounds and as versatile building blocks for further …