Stereocontrol in Conformationally Stable C(sp <sup>2</sup> )─C(sp <sup>3</sup> ) Atropisomers

A Antoine Domain (Aix Marseille Univ, CNRS, Centrale Med, iSm2 Marseille France) G Guishun Bai (College of Pharmaceutical Science &amp; Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals Zhejiang University of Technology Hangzhou 310014 P.R. China) J Juan‐Carlos Castillo (Escuela de Ciencias Químicas Universidad Pedagógica y Tecnológica de Colombia Avenida Central del Norte 39‐115 Tunja Colombia) H Hassane Moussa Abdraman (Aix Marseille Univ, CNRS, Centrale Med, iSm2 Marseille France) S Stéphane Humbel (Aix Marseille Univ, CNRS, Centrale Med, iSm2 Marseille France) M Michel Giorgi (Aix‐Marseille Univ, CNRS Centrale Méditerranée Marseille FSCM France) J Jean‐Valère Naubron (Aix Marseille Université, CNRS, Centrale Med, FSCM, Spectropole Marseille France) S Sara Chentouf (Aix Marseille Université, CNRS, Centrale Med, FSCM, Spectropole Marseille France) J Jean Rodriguez (Aix Marseille Univ, CNRS, Centrale Med, iSm2 Marseille France) X Xiaoze Bao D Damien Bonne (Aix Marseille Univ, CNRS, Centrale Med, iSm2 Marseille France)

Abstract

Abstract We report a two‐step sequence for the enantioselective construction of a rare family of stable C(sp 2 )─C(sp 3 ) atropisomers featuring two additional stereogenic centers. The process begins with an organocatalyzed dihydrobenzofurannulation that establishes and controls the stereochemistry of two carbon centers, followed by a highly diastereoselective functionalization that significantly enhances the barrier to diastereomerization of the C(sp 2 )─C(sp 3 ) bond, effectively locking and stabilizing its configuration.

Article Details

Volume / Issue Vol. 64, Issue 28
Published July 07, 2025
ISSN 1433-7851
Publisher Wiley

Journal Info

Angewandte Chemie International Edition

Wiley

ISSN: 1433-7851 Physical Sciences

Authors (11)

A

Antoine Domain

Aix Marseille Univ, CNRS, Centrale Med, iSm2 Marseille France

G

Guishun Bai

College of Pharmaceutical Science &amp; Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals Zhejiang University of Technology Hangzhou 310014 P.R. China

J

Juan‐Carlos Castillo

Escuela de Ciencias Químicas Universidad Pedagógica y Tecnológica de Colombia Avenida Central del Norte 39‐115 Tunja Colombia

H

Hassane Moussa Abdraman

Aix Marseille Univ, CNRS, Centrale Med, iSm2 Marseille France

S

Stéphane Humbel

Aix Marseille Univ, CNRS, Centrale Med, iSm2 Marseille France

M

Michel Giorgi

Aix‐Marseille Univ, CNRS Centrale Méditerranée Marseille FSCM France

J

Jean‐Valère Naubron

Aix Marseille Université, CNRS, Centrale Med, FSCM, Spectropole Marseille France

S

Sara Chentouf

Aix Marseille Université, CNRS, Centrale Med, FSCM, Spectropole Marseille France

J

Jean Rodriguez

Aix Marseille Univ, CNRS, Centrale Med, iSm2 Marseille France

X

Xiaoze Bao

D

Damien Bonne

Aix Marseille Univ, CNRS, Centrale Med, iSm2 Marseille France