- Efficient synthesis of chiral benzofuryl β-amino alcohols via a catalytic asymmetric Henry reaction
-
Chiral β-amino alcohol ligands were found effective for the copper(ii)-catalyzed asymmetric Henry reaction of benzofuran-2-carbaldehydes with nitromethane, which led to the formation of (S)-enriched benzofuryl β-nitro alcohols with satisfactory enantioselectivities (up to 98% ee). Using this catalytic protocol, bioactive (S)-benzofuryl β-amino alcohols could be conveniently prepared in short steps.
- Chen, Wei,Zhou, Zhao-Hui,Chen, Hong-Bin
-
supporting information
p. 1530 - 1536
(2017/02/15)
-
- S1P RECEPTORS MODULATORS
-
The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
- -
-
Page/Page column 67
(2010/04/30)
-
- New scaffolds for the design of selective estrogen receptor modulators
-
In the present work we report the synthesis of four new ER ligands which can be used as scaffolds for the introduction of the basic side chains necessary for antiestrogenic activity. Affinities and agonist/antagonist characterization of the ligands for both ERα and ERβ have been determined in a competitive radioligand assay, and in an in vitro coactivator recruitment functional assay, respectively. Molecular modelling techniques have been used in order to rationalize the experimental results. Compound 2 is reported as a novel ERβ-agonist/ERα-antagonist. Two compounds show an interesting antitumour profile towards two pancreatic cancer cell lines and have been selected for in vivo assays.
- Martin-Santamaria, Sonsoles,Rodriguez, Jose-Juan,De Pascual-Teresa, Sonia,Gordon, Sandra,Bengtsson, Martin,Garrido-Laguna, Ignacio,Rubio-Viqueira, Belen,Lopez-Casas, Pedro P.,Hidalgo, Manuel,De Pascual-Teresa, Beatriz,Ramos, Ana
-
experimental part
p. 3486 - 3496
(2009/02/05)
-
- A Novel Synthesis of Benzofuran and Related Compounds. III. The Vilsmeier Reaction of Phenoxyacetaldehyde Diethyl Acetals
-
A novel synthesis of 2-benzofurancarbaldehydes by the Vilsmeier reaction of phenoxyacetaldehyde diethyl acetals is described.
- Hirota, Takashi,Fujita, Hiroko,Sasaki, Kenji,Namba, Tetsuto
-
p. 1715 - 1716
(2007/10/02)
-
- Synthesis of 2-amino-4-(2-benzofuryl)Δ1 pyrrolines and study of their antidysrhythmic properties
-
The synthesis of 2-amino 4(2-benzofuryl)Δ1 pyrrolines, substituted in the aromatic ring and/or on the nitrogen atom of the amino group, is described. These derivatives are obtained from 3 (2-benzofuryl) acrylic esters, on which nitromethane is added. The reduction of 4-nitrobutyric esters lead to pyrrolidinones, and then to the entitled derivatives. Some analogs, the benzofuran ring of which is replaced by another heterocycle, were also prepared. Some of them exhibit interesting antidysrhythmic properties.
- Maillard,Langlois,Vo Van,et al.
-
p. 353 - 358
(2007/10/02)
-