1223573-23-6Relevant articles and documents
Production method of baricitinib
-
Paragraph 0038-0039, (2019/10/04)
The invention relates to a production method of baricitinib. The production method of the baricitinib comprises the steps of using N-tert-butoxycarbonyl-4-piperidone as an initial raw material, subjecting the N-tert-butoxycarbonyl-4-piperidone and a Wittig-Horner agent to a condensation reaction to obtain 3-(2-oxymethylene)-1-azetidinecarboxylicacidtert-butylester, and then subjecting the 3-(2-oxymethylene)-1-azetidinecarboxylicacidtert-butylester and 4-pyrazoleboronic acid pinacol ester to a Michael addition reaction; subjecting an obtained pinacol ester intermediate and a 4-chlorobenzopyrimidine derivative to a cross-coupling reaction under the action of a metal catalyst; and finally, converting R1 into a cyano group through functional group conversion, and conducting removal, protection and the like to complete production of the baricitinib.
SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS
-
Paragraph 0670; 0671, (2017/04/04)
Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
SUBSTITUTED BENZOTHIOPHENYL DERIVATIVES AS GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
-
Page/Page column 150-151, (2016/05/02)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) wherein R1, R2, R3, R5, R6, W, and A are defined herein.