Protected propargylic acetals. Nicholas–Prins cyclization leading to functionalized 2-alkynyl-tetrahydropyrans. Intramolecular trapping by allenes
作者:Clarisse Olier、Stéphane Gastaldi、Gérard Gil、Michèle P. Bertrand
DOI:10.1016/j.tetlet.2007.09.021
日期:2007.10
Dicobalt hexacarbonyl complexes derived from propargylic acetals undergo Lewis acid-mediated Nicholas–Prins cyclization in the presence of homoallylic alcohols. The trapping of the resulting cyclic carbocation enables the synthesis of a series of functionalizedtetrahydropyrans. The complexation of the triple bond contributes to the suppression of the side reactions and very significantly increases
[EN] PROCESS FOR THE MANUFACTURE OF CARBOXAMIDES<br/>[FR] PROCÉDÉ DE FABRICATION DE CARBOXAMIDES
申请人:SOLVAY
公开号:WO2017140593A1
公开(公告)日:2017-08-24
The present invention concerns a process for the manufacture of carboxamides, in particular agrochemical or pharmaceutically active ingredients, from pyrazole ketone compounds.
本发明涉及一种从吡唑酮化合物制备羧酰胺的方法,特别是用于农药或药用活性成分。
[EN] MANUFACTURE OF HYDRAZINYL COMPOUNDS USEFUL IN THE MANUFACTURE OF PYRAZOLE CARBOXYLIC ACID AND DERIVATIVES, HYDRAZINYL COMPOUNDS AND THEIR USE<br/>[FR] FABRICATION DE COMPOSÉS HYDRAZINYLE UTILES DANS LA FABRICATION D'ACIDE PYRAZOLE CARBOXYLIQUE ET DE DÉRIVÉS, COMPOSÉS HYDRAZINYLE ET LEUR UTILISATION
申请人:SOLVAY
公开号:WO2018024644A1
公开(公告)日:2018-02-08
The present invention concerns the manufacture of hydrazinyl compounds useful in the manufacture of pyrazole carboxylic acid and derivatives thereof and processes for the manufacture of agrochemical or pharmaceutical compounds. The invention also concerns hydrazinyl compounds and their use.
There are provided compounds of the general formulas
wherein X, Y, R1, R2, R3, R4 and R5 are as described herein. The compounds exhibit anticancer activity.
Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists
作者:HyungChul Ryu、Sejin Seo、Jee-Young Lee、Tae-Hwan Ha、Sunho Lee、Aeran Jung、Jihyae Ann、Sung-Eun Kim、Suyoung Yoon、Mannkyu Hong、Peter M. Blumberg、Robert Frank-Foltyn、Gregor Bahrenberg、Klaus Schiene、Hannelore Stockhausen、Thomas Christoph、Sven Frormann、Jeewoo Lee
DOI:10.1016/j.ejmech.2015.02.001
日期:2015.3
A series of pyridine derivatives in the C-region of N-((6-trifluoromethyl-pyridin-3-yl)methyl) 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. The SAR analysis indicated that 6-difluorochloromethyl pyridine derivatives were the best surrogates of the C-region for previous leads. Among them, compound 31 showed excellent antagonism to capsaicin as well as to multiple hTRPV1 activators. It demonstrated strong analgesic activity in the formalin test in mice with full efficacy and it blocked capsaicin-induced hypothermia in vivo. (C) 2015 Elsevier Masson SAS. All rights reserved.