Title:
カルボニルの不斉アルキル化
Document Type and Number:
Japanese Patent JP5081163
Kind Code:
B2
Abstract:
This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.
Inventors:
Albert, Martin
Shutoulm, Hubert
Berger, Andreas
Kreminger, Peter
Shutoulm, Hubert
Berger, Andreas
Kreminger, Peter
Application Number:
JP2008550696A
Publication Date:
November 21, 2012
Filing Date:
January 22, 2007
Export Citation:
Assignee:
SANDOZ AKTIENGESELLSCHAFT
International Classes:
C07C253/30; C07C255/53; C07C255/56; C07F5/02; C07B53/00
Domestic Patent References:
| JP2005247710A |
Attorney, Agent or Firm:
Yoshio Kawaguchi
Makoto Ono
Chihiro Watanabe
Kenkyo Kanayama
Katsuma Osaki
Mitsuaki Tsubokura
Makoto Ono
Chihiro Watanabe
Kenkyo Kanayama
Katsuma Osaki
Mitsuaki Tsubokura