2068065-63-2Relevant academic research and scientific papers
Regioselective Synthesis of Pyrazolo[1,5- a]pyridine via TEMPO-Mediated [3 + 2] Annulation-Aromatization of N-Aminopyridines and α,β-Unsaturated Compounds
Wang, Amu,Liu, Ya-Zhou,Shen, Zhongke,Qiao, Zeen,Ma, Xiaofeng
supporting information, p. 1454 - 1459 (2022/03/01)
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.
PYRAZOLOPYRIDINE COMPOUND AS RET INHIBITOR AND APPLICATION THEREOF
-
Paragraph 0249; 0255-0257, (2022/02/19)
Disclosed is a series of pyrazolopyridine compounds, and application thereof in the preparation of RET kinase inhibitors for treatment. Specifically disclosed is the compound represented by formula (I), or a pharmaceutically acceptable salt thereof.
Pyrazolopyridine derivatives for regulating synthesis activity of estrogen receptor
-
Paragraph 0220-0227, (2021/09/15)
The invention relates to the technical field of organic chemistry and medicinal chemistry, and in particular, relates to pyrazolopyridine derivatives for regulating the synthesis activity of an estrogen receptor. According to the specific technical scheme, under the alkaline condition, substituted 1-aminopyridine and an alpha,beta-unsaturated compound are stirred together in the presence of an oxidizing agent, and the substituted pyrazol[1,5-a]pyridine compounds are formed. A one-step synthesis strategy is adopted, the alpha,beta-unsaturated compound is used as a raw material, and a series of pyrazol[1,5-a]pyridine compounds are efficiently and highly selectively synthesized in the presence of an organic oxidant.
Aliphatic ring derivatives as RET inhibitors
-
, (2020/09/08)
The invention discloses a series of compounds with aliphatic ring structures and application of the compounds in preparation of RET kinase inhibitors. Specifically disclosed are a compound representedby formula (I), an isomer thereof, or a pharmaceuticall
PROCESS FOR THE PREPARATION OF 6-(2-HYDROXY-2-METHYLPROPOXY)-4-(6-(6-((6-METHOXYPYRIDIN-3-YL)METHYL)-3,6-DIAZABICYCLO[3.1.1]HEPTAN-3-YL)PYRIDIN-3-YL)PYRAZOLO[1,5-A]PYRIDINE-3-CARBONITRILE
-
, (2019/04/25)
In some embodiments, provided herein is a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof, as disclosed herein.
FORMULATIONS COMPRISING 6-(2-HYDROXY-2-METHYLPROPOXY)-4-(6-(6-((6-METHOXYPYRIDIN-3-YL)METHYL)-3,6-DIAZAB ICYCLO[3.1.1]HEPTAN-3-YL)PYRIDIN-3-YL)PYRAZOLO[1,5-A]PYRIDINE-3-CARBONITRILE
-
Page/Page column 322; 323, (2019/05/06)
6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile, or a pharmaceutically acceptable salt, amorphous form, polymorph form, or pharmaceutical composition (including solid formulations or liquid formulations) thereof and the use thereof for treating diseases and disorders which can be treated with a RET kinase inhibitor, such as RET-associated diseases and disorders, e.g., proliferative disorders such as cancers, including hematological cancers and solid tumors, and gastrointestinal disorders such as IBS are disclosed.
SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS
-
Paragraph 001815, (2017/02/09)
Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.
