Search results for "Conjugate"
showing 10 items of 644 documents
Copper-catalysed enantioselective Michael addition of malonic esters to β-trifluoromethyl-α,β-unsaturated imines
2017
[EN] Copper triflate-BOX complexes catalyse the enantioselective conjugate addition of methyl malonate to beta-trifluoromethyl-alpha,beta-unsaturated imines to give the corresponding enamines bearing a trifluoromethylated stereogenic centre with good yields, and diastereo- and enantioselectivities. The usefulness of the method has been shown with the synthesis of optically active beta-trifluoromethyl delta-amino esters and optically active trifluoromethyl piperidones.
Catalytic Enantioselective Conjugate Alkynylation of α,β-Unsaturated 1,1,1-Trifluoromethyl Ketones with Terminal Alkynes.
2016
The first catalytic enantioselective conjugate alkynylation of α,β-unsaturated 1,1,1-trifluoromethyl ketones has been carried out. Terminal alkynes and 1,3-diynes were treated with trifluoromethyl ketones in the presence of a low catalytic load of a CuI-MeOBIPHEP complex (2.5 mol %) and triethylamine (10 mol %) to give the corresponding trifluoromethyl ketones bearing a propargylic stereogenic center at the β position with good yields and excellent enantiomeric excesses in most of the cases. No 1,2-addition products were formed under the reaction conditions. The procedure showed broad substrate scope for alkyne, diyne, and enone. A rationale for the observed stereochemistry has been provide…
Catalytic asymmetric conjugate addition of terminal alkynes to β-trifluoromethyl α,β-enones.
2014
The first enantioselective conjugate alkynylation of β-trifluoromethyl α,β-enones using terminal alkynes and a taniaphos–Cu(I) complex as catalyst is described. Ketones bearing a trifluoromethylated propargylic chiral centre in the β-position were obtained with good yields and high enantiomeric excesses (up to 99%).
Highly enantioselective copper(I)-catalyzed conjugate addition of 1,3-diynes to a,b-unsaturated trifluoromethyl ketones
2015
[EN] The conjugate diynylation of a,b-unsaturated trifluoromethyl ketones is carried out in the presence of a low catalytic load (2.5 mol%) of a copper(I)–MeOBIPHEP complex, triethylamine and a terminal 1,3-diyne. Pre-metalation of the terminal 1,3-diyne with stoichiometric or higher amounts of dialkylzinc reagent is not required. The corresponding internal diynes bearing a propargylic stereogenic center are obtained with good yields and excellent enantioselectivities.
Highly enantioselective copper(I)-catalyzed conjugate addition of terminal alkynes to 1,1-difluoro-1-(phenylsulfonyl)-3-en-2-ones: new ester/amide su…
2013
A highly enantioselective copper-catalyzed conjugate alkynylation of monoactivated enones, namely 1,1-difluoro-1-(phenylsulfonyl)-3-en-2-ones, is described. The reaction products are obtained with good yields and excellent enantioselectivities (from 92 to 99% ee). The β-alkynylated difluoro(phenylsulfonyl) ketones can be converted into the corresponding β-alkynylated difluoro- and trifluoromethyl ketones, esters and amides. This is the first example on the use of 1,1-difluoro-1-(phenylsulfonyl)-3-en-2-ones as substrates in an enantioselective reaction, which have been shown to be new ester/amide surrogates.
Application of tris-allyl-DOTA in the preparation of DOTA–peptide conjugates
2006
Abstract The synthesis of tris-allyl-DOTA starting from cyclen and its application in the preparation of DOTA–peptide conjugates is reported. Clinically important conjugates such as DOTA–Tyr3-octreotide (DOTA–TOC), DOTA–Tyr3-octreotate (DOTA–TATE) as well as a DOTA–RGD peptide were synthesized in high yields with Fmoc solid phase peptide synthesis. The final, extremely reliable de-allylation was achieved on solid phase by different methods identifying morpholine/Pd(0) as the most suitable one obtaining all DOTA peptide conjugates in high yields. All DOTA–peptides were purified by reversed phase HPLC and structural identity was proved using MALDI-TOF mass spectrometry.
A Short Synthesis of Polysubstituted Pyrrolidines via α-(Alkylideneamino)nitriles
2004
α-(Alkylideneamino)nitriles can be deprotonated under mild conditions. Their conjugated anions react with enones in a 1,4-addition to yield δ-keto-α-(alkylideneamino)nitriles which in turn can be reduced to form pyrrolidines in a one-pot reaction sequence.
Spectral rigidity and invariant distributions on Anosov surfaces
2014
This article considers inverse problems on closed Riemannian surfaces whose geodesic flow is Anosov. We prove spectral rigidity for any Anosov surface and injectivity of the geodesic ray transform on solenoidal 2-tensors. We also establish surjectivity results for the adjoint of the geodesic ray transform on solenoidal tensors. The surjectivity results are of independent interest and imply the existence of many geometric invariant distributions on the unit sphere bundle. In particular, we show that on any Anosov surface $(M,g)$, given a smooth function $f$ on $M$ there is a distribution in the Sobolev space $H^{-1}(SM)$ that is invariant under the geodesic flow and whose projection to $M$ i…
Improving the Frying Performance and Oxidative Stability of Refined Soybean Oil by Tocotrienol-Rich Unsaponifiable Matters of Kolkhoung (Pistacia khi…
2018
Increasing consumer awareness for all natural products has quickly led to growing research on new resources of potent and profitable natural antioxidants. In this context, for the first time, the Kolkhoung hull oil (KHO) (Pistacia khinjuk)-unsaponifiable matters (USM) (UHO) (100, 200, and 400 mg kg−1) were incorporated into refined soybean oil (RSO) and the oxidative stability of prepared oils was measured during 32 hours of frying. Then, the obtained results (oxidative stability) were compared to the samples containing tert-butyl hydroquinone (TBHQ) (100 mg kg−1) as a common synthetic antioxidant. According to the results of oxidative stability assays of acid values, conjugated diene value…
Thermal Induction of 9t12t Linoleic Acid: a New Pathway for the Formation of Conjugated Linoleic Acids
2009
Accepted version of an article published in the journal: International Journal of Engineering and Technology Published version available at: http://www.ijetch.org/papers/066.pdf Thermal induction of 9t12t fatty acid leading to the formation of Conjugated Linoleic Acids (CLA) has been demonstrated by subjecting glyceride, and methyl ester of the acid to heat treatment. Fifteen micro liter portions of the glyceride sample containing 9t12t fatty acid (trilinoelaidin) were placed in micro glass ampoules and sealed under nitrogen and then subjected to thermal treatment at 250oC. The glass ampoules were taken out at regular time intervals, and the contents were subjected to composition analysis b…