METHOD FOR PRODUCING 18F-LABELED COMPOUND AND HIGH MOLECULAR COMPOUND TO BE USED IN THE METHOD
申请人:Takahashi Takashi
公开号:US20120329968A1
公开(公告)日:2012-12-27
The present invention aims at solving the problems of conventional methods for producing an
18
F-labeled compound, that is, the problem of purification of a compound in a liquid phase synthesis method and the problem of an insufficient yield due to the reduction of reactivity in a solid phase synthesis method. There is provided a method for producing an
18
F-labeled compound including: allowing a high molecular compound containing a residue of a precursor compound to be labeled and a residue of a phase transfer catalyst in the molecule thereof to react with
18
F
−
; and removing the
18
F-labeled compound from the high molecular compound.
Gold(I)-Catalyzed Intramolecular Dihydroamination of Allenes with <i>N</i>,<i>N</i>′-Disubstituted Ureas To Form Bicyclic Imidazolidin-2-ones
作者:Hao Li、Ross A. Widenhoefer
DOI:10.1021/ol900730w
日期:2009.6.18
mixture of gold(I) N-heterocyclic carbene complex (5)AuCl [5 = 1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidine] and AgPF6 at room temperature for 2 h led to isolation of bicyclic imidazolidin-2-one 4 in 93% yield with ≥98% diastereomeric purity. Gold-catalyzed dihydroamination was effective for a number of N-δ- and N-γ-allenyl ureas to form the corresponding bicyclic imidazolidin-2-ones in good yield
Combining Gold(I)/Gold(III) Catalysis and CH Functionalization: A Formal Intramolecular [3+2] Annulation towards Tricyclic Indolines and Mechanistic Studies
Gold rush: A combination of oxidative gold(I)/gold(III) catalysis and CHfunctionalization led to the first oxidative coupling between in situ generated alkyl gold reagents and CH bonds, affording tricyclic indolines through a formal [3+2] annulation between a vinyl group and an aniline moiety [see scheme; Tf=trifluoromethanesulfonyl, Selectfluor=1‐chloromethyl‐4‐fluoro‐1,4‐diazoniabicyclo[2.2.2]octane
METHODE FOR PRODUCING F-LABELLED COMPOUND AND HIGH MOLECULAR COMPOUND TO BE USED IN THE METHOD
申请人:Tokyo Institute of Technology
公开号:EP2537854A1
公开(公告)日:2012-12-26
The present invention aims at solving the problems of conventional methods for producing an 18F-labeled compound, that is, the problem of purification of a compound in a liquid phase synthesis method and the problem of an insufficient yield due to the reduction of reactivity in a solid phase synthesis method. There is provided a method for producing an 18F-labeled compound including: allowing a high molecular compound containing a residue of a precursor compound to be labeled and a residue of a phase transfer catalyst in the molecule thereof to react with 18F-; and removing the 18F-labeled compound from the high molecular compound.
Solid-supported reagents composed of a copolymer possessing 2- O -sulfonyl mannosides and phase-transfer catalysts for the synthesis of 2-fluoroglucose
We described the synthesis of a solid-supported co-polymer possessing mannosides and phase-transfer catalysts and synthesis of 2-fluoroglucoside from it. We first prepared a soluble copolymer from two allene monomers possessing a precursor for the synthesis of 2-fluoroglycose and a crown ether. The copolymerization of the monomers via the pi-ally nickel-catalyst smoothly proceeded at room temperature to provide a desired copolymer without decomposition of the sulfonate esters. The copolymer exhibited high reactivity towards fluorination in comparison with a conventional precursor. We next synthesized the solid-supported copolymer by using the solid-supported initiator attached with TentaGel (R) resins. TentaGel (R) enabled polymerization under stirring with stirring bar without decomposition. The solid-supported copolymer exhibited comparable reactivity towards fluorination in comparison with the soluble copolymer. In addition, it can be easily separated from the reaction vessel by filtration. (C) 2015 Elsevier Ltd. All rights reserved.