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

2019 ◽  
Vol 10 (48) ◽  
pp. 11141-11146 ◽  
Author(s):  
Sándor B. Ötvös ◽  
Miquel A. Pericàs ◽  
C. Oliver Kappe

The continuous flow synthesis of the chiral key intermediate of (−)-paroxetine is demonstrated via a solvent-free organocatalytic conjugate addition followed by a telescoped reductive amination–lactamization–amide/ester reduction sequence.

Author(s):  
Lais S. D. Azevedo ◽  
Anderson R. Aguillon ◽  
Marcelo T. Lima ◽  
Raquel A. C. Leão ◽  
Rodrigo O. M. A. de Souza

Author(s):  
Xiaojun Wei ◽  
Stephen V. Kershaw ◽  
Xiaodan Huang ◽  
Mingxia Jiao ◽  
Chau Chun Beh ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 2040
Author(s):  
Zsolt Fülöp ◽  
Péter Bana ◽  
István Greiner ◽  
János Éles

A new, continuous-flow consecutive reduction method was developed for the C-N bond formation in the synthesis of the key intermediate of the antipsychotic drug cariprazine. The two-step procedure consists of a DIBAL-H mediated selective ester reduction conducted in a novel, miniature alternating diameter reactor, followed by reductive amination using catalytic hydrogenation on 5% Pt/C. The connection of the optimized modules was accomplished using an at-line extraction to prevent precipitation of the aluminum salt byproducts.


Author(s):  
Carsten J. Schmiegel ◽  
Patrik Berg ◽  
Franziska Obst ◽  
Roland Schoch ◽  
Dietmar Appelhans ◽  
...  

2021 ◽  
Vol 27 (18) ◽  
pp. 5653-5657 ◽  
Author(s):  
Andreas Simoens ◽  
Thomas Scattolin ◽  
Thibault Cauwenbergh ◽  
Gianmarco Pisanò ◽  
Catherine S. J. Cazin ◽  
...  

1999 ◽  
Vol 23 (9) ◽  
pp. 574-575
Author(s):  
Firouz Matloubi Moghaddam ◽  
Mohammad Ghaffarzadeh ◽  
Seyed Hossein Abdi-Oskoui

An AICl3–ZnCl2 mixture supported on silica gel is found to be an efficient medium for the Fries rearrangement of acyloxybenzene or naphthalene derivatives in solvent-free conditions under microwave irradiation.


2021 ◽  
pp. 2101616
Author(s):  
Iñigo Torres ◽  
Marta Alcaraz ◽  
Roger Sanchis‐Gual ◽  
Jose A. Carrasco ◽  
Michael Fickert ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 303
Author(s):  
András Gy. Németh ◽  
Renáta Szabó ◽  
György Orsy ◽  
István M. Mándity ◽  
György M. Keserű ◽  
...  

We have developed the continuous-flow synthesis of thioureas in a multicomponent reaction starting from isocyanides, amidines, or amines and sulfur. The aqueous polysulfide solution enabled the application of sulfur under homogeneous and mild conditions. The crystallized products were isolated by simple filtration after the removal of the co-solvent, and the sulfur retained in the mother liquid. Presenting a wide range of thioureas synthesized by this procedure confirms the utility of the convenient continuous-flow application of sulfur.


Sign in / Sign up

Export Citation Format

Share Document