Trichlorophenol (TCP) sulfonate esters: A selective alternative to pentafluorophenol (PFP) esters and sulfonyl chlorides for the preparation of sulfonamides
METHOD OF PREPARING TAXANE DERIVATIVES AND INTERMEDIATES USED THEREIN
申请人:Kim Nam Du
公开号:US20100317868A1
公开(公告)日:2010-12-16
The present invention relates to a novel method of preparing a taxane derivative having an anti-tumor and anti-leukemia activity, and intermediates used therein.
本发明涉及一种制备具有抗肿瘤和抗白血病活性的紫杉醇衍生物的新方法,以及其中使用的中间体。
[EN] NOVEL COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS
申请人:CHIESI FARMA SPA
公开号:WO2014095700A1
公开(公告)日:2014-06-26
This invention relates to heterocyclic compounds, which are pyrimidinone derivatives having human neutrophil elastase inhibitory properties, and their use in therapy.
[EN] FLUORINATION METHOD<br/>[FR] PROCÉDÉ DE FLUORATION
申请人:ISIS INNOVATION
公开号:WO2015140572A1
公开(公告)日:2015-09-24
The present invention relates to a process for producing an organic compound comprising an 18F atom. The compounds comprising an 18F can be useful as PET ligands for use in diagnostics and/or scanning. The process of the invention comprises treating an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp2 hybridised carbon atom, with (i) 18F – and (ii) a copper compound. The invention also provides the use of an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp2 hybridised carbon atom, in a process for producing an organic compound comprising an 18F atom, which process comprises treating the organoboron compound with (i) 18F – and (ii) a copper compound. The invention also provides a compound of formula (XXXVII): wherein: each PGA is independently H or an alcohol protecting group; PGB is H or a carboxylic acid protecting group; each PGC is independently an amine protecting group; Z is a group selected from a boronic ester group, a boronic acid group, a borate group, and a trifluoroborate group; and a is an integer from 0 to 4.
PROCESS FOR PRODUCTION OF BIS-QUATERNARY AMMONIUM SALT, AND NOVEL INTERMEDIATE
申请人:Okamoto Kuniaki
公开号:US20120130107A1
公开(公告)日:2012-05-24
Object To provide a method for producing a bis-quaternary ammonium salt efficiently and a novel synthetic intermediate thereof.
Solution The present invention relates to a method for producing a bis-quaternary ammonium salt represented by a general formula [3] which comprises reacting a disulfonic acid ester represented by a general formula [1] (in the formula, definitions of two R
1
's and T are as described in claim
1
) with a tertiary amine represented by a general formula [2] (in the formula, definitions of R
3
to R
5
are as described in claim
1
), and a disulfonic acid ester represented by a general formula [1′] (in the formula, two R
16
's represent independently a halogen atom or a C1-C3 fluoroalkyl group, and two m's represent independently an integer of 1 to 5).
Process for the Preparation of Leukotriene Receptor Antagonist (Montelukast Sodium)
申请人:Ray Uttam Kumar
公开号:US20090326232A1
公开(公告)日:2009-12-31
The present invention relates to an improved process for the preparation of [R-(E)]-1-[[[1-[3-[2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]-cyclopropaneacetic acid, monosodium salt of Formula (I).