- Regioselective Synthesis of Pyrazolo[1,5- a]pyridine via TEMPO-Mediated [3 + 2] Annulation-Aromatization of N-Aminopyridines and α,β-Unsaturated Compounds
-
A TEMPO-mediated [3 + 2] annulation-aromatization protocol for the preparation of pyrazolo[1,5-a]pyridines from N-aminopyridines and α,β-unsaturated compounds was developed. The procedure offered multisubstituted pyrazolo[1,5-a]pyridines in good to excellent yield with high and predictable regioselectivity. The modification of marketed drugs including Loratadine, Abiraterone, and Metochalcone, and a one-pot three-step gram scale synthesis of key intermediate for the preparation of Selpercatinib were demonstrated. Mechanism studies show that TEMPO serves both as a Lewis acid and as an oxidant.
- Liu, Ya-Zhou,Ma, Xiaofeng,Qiao, Zeen,Shen, Zhongke,Wang, Amu
-
-
- SUBSTITUTED FUSED AROMATIC RING DERIVATIVE, COMPOSITION AND USE THEREOF
-
Provided are a substituted fused aromatic ring derivative, a composition containing the compound, and a use thereof. The substituted fused aromatic ring derivative is a compound represented by formula (I) or a tautomer, stereoisomer, prodrug, crystal form, pharmaceutically acceptable salt, hydrate or solvate thereof. The compound and the composition can be used to treat various protein tyrosine kinase-mediated diseases or disorders.
- -
-
Paragraph 0183-0185
(2021/11/04)
-
- In Situ Preparation and Consumption of O -Mesitylsulfonylhydroxylamine (MSH) in Continuous Flow for the Amination of Pyridines
-
The paper demonstrates a safe method in which highly unstable O -mesitylsulfonylhydroxylamine (MSH) can be prepared and consumed in continuous flow. MSH was prepared in situ and used for the flow amination of a range of pyridines, which were subsequently transformed into useful pyrazolopyridine building blocks.
- Brocklehurst, Cara E.,Koch, Guido,Rothe-P?llet, Stephanie,La Vecchia, Luigi
-
supporting information
p. 1636 - 1640
(2017/08/11)
-
- PYRAZOLOPYRIDINE DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF
-
A pyrazolopyridine derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof exhibits a strong EP1 receptor antagonistic effect. Thus, the derivative or the pharmacologically acceptable salt is useful as
- -
-
Paragraph 0423; 0424
(2014/01/07)
-
- Structure-kinetics relations holding in the amination of six-membered nitrogen-containing heterocyclic compounds
-
Relative rates of the amination of 3-X- and 4-X-substituted pyridines (X = H, 3-Me, 4-Me, 3-F3C, 3-CN, 4-CN, 3-Cl, 3-Br, 4-MeO, 4-Me 2N), pyrazine, quinoline, isoquinoline, 2,2′- and 4,4′-bipyridines, and 1,10-phenanthroline with O-
- Borodkin,Vorob'ev,Shubin
-
experimental part
p. 897 - 903
(2011/10/04)
-
- SYNTHESES AND TRANSFORMATIONS OF SOME HETEROCYCLIC HYDROXYLAMINES
-
Syntheses of some hydroxylaminoazines, their quaternized derivatives or N-oxides and N-amino compounds are described.Several transformations of these compounds and cyclization reactions are presented.
- Tomazic, Alenka,Tisler, Miha,Stanovnik, Branko
-
p. 1787 - 1794
(2007/10/02)
-