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Papers by joakim löfstedt
European Journal of Organic Chemistry, Dec 1, 1999
In Scheme 4 on page 3278, structures 5a and 5b are incorrectly given. The correct scheme is print... more In Scheme 4 on page 3278, structures 5a and 5b are incorrectly given. The correct scheme is printed below. Scheme 4. (a) Pd/C, H 2 , MeOH; (b) pyridineϪSO 3 , DMSO, Et 3 N, CH 2 Cl 2 ; (c) 9, tBuOK, THF, Ϫ78°C; (d) PtO 2 , H 2 , EtOH; (e) Na/NH 3 , EtOH, Ϫ78°C to room temp.; (f) 10%
Journal of Organic Chemistry, Nov 1, 2001
Regio-and stereoselective palladium-catalyzed reactions of allene-substituted 1,3-dienes 1 in ace... more Regio-and stereoselective palladium-catalyzed reactions of allene-substituted 1,3-dienes 1 in acetic acid at room temperature lead to cyclization with formation of a carbon-carbon bond between the middle carbon of the allene and the terminal carbon of the 1,3-diene. Two different types of reactions, both that constitute 1,4-carboacetoxylations of the 1,3-diene, have been developed. In one of the reactions, Pd(II) catalyzes the oxidation of 1 to bicyclic compounds 2, and in the other, Pd(0) catalyzes the transformation of 1 to bicyclic compounds 3. The products 2 are useful for further synthetic transformations and undergo Diels-Alder reactions with dienophiles to give polycyclic ring systems.
L'invention concerne un compose de formule (I), dans laquelle G est un cycle pyrazole tel que... more L'invention concerne un compose de formule (I), dans laquelle G est un cycle pyrazole tel que defini dans la description et R 4 , R 5 , R 6 et R 7 sont tels que definis dans la description ; ou un de ses esters, amides, solvates ou sels pharmaceutiquement acceptables, y compris un sel d'un tel ester ou amide, et un solvate d'un tel ester, amide ou sel. L'invention concerne egalement l'utilisation de tels composes pour le traitement ou la prophylaxie d'un etat associe avec une maladie ou un trouble associe avec l'activite du recepteur d'estrogene.
ChemSusChem, 2021
By extracting lignin, pulp production can be increased without heavy investments in a new recover... more By extracting lignin, pulp production can be increased without heavy investments in a new recovery boiler, the typical bottleneck of a pulp mill. The extraction is performed by using 0.20 and 0.15 weight equivalents of CO 2 and H 2 SO 4 respectively. Herein, we describe lignin esterification with fatty acids using benign reagents to generate a lignin ester mixable with gas oils. The esterification is accomplished by activating the fatty acid and lignin with acetic anhydride which can be regenerated from the acetic acid recycled in this reaction. The resulting mass balance ratio is fatty acid/lignin/acetic acid (2 : 1 : 0.1). This lignin ester can be hydroprocessed to generate hydrocarbons in gasoline, aviation, and diesel range. A 300-hour continuous production of fuel was accomplished. By recirculating reagents from both the esterification step and applying a water gas shift reaction on off-gases from the hydroprocessing, a favorable overall mass balance is realized.
Lagga socken är ett arkeologiskt intressant område med många fornlämningar från järnåldern. Stran... more Lagga socken är ett arkeologiskt intressant område med många fornlämningar från järnåldern. Strandförskjutningen har förändrat området över tid. Långhundraleden, en viktig forntida vattenled, går genom området och är central för att förstå utvecklingen av området. Området låg i Attundaland men var en gränstrakt till Tiundaland. I Tiundaland ligger Gamla Uppsala som påverkat området. Extra stora gravhögar, så kallade storhögar, är många på en liten yta. Det finns också storhögar som är demolerade, men kan hittas på historiska kartor. Kashögen är en av dessa försvunna högar. Kashögen ligger vid Kasby och förledet i ortnamnet, -Kas, är förknippat med vårdkase och varningseldar som användes för kommunikation och varning ifall fiender var i annalkande.Uppsatsen beskriver Kashögen som att vara den första, den största och den storhög som initierar att de andra storhögarna i området byggs
Selective palladium-catalyzed 1,4-functionalization : allenes and dienes in palladium chemistry a... more Selective palladium-catalyzed 1,4-functionalization : allenes and dienes in palladium chemistry and total syntheses of (+)-pseudoconhydrine and (+)-monomorine I
Journal of medicinal chemistry, Jan 21, 2018
The nuclear hormone receptor RORC2 (also known as RORγt) is a promising target for the treatment ... more The nuclear hormone receptor RORC2 (also known as RORγt) is a promising target for the treatment of autoimmune diseases. A small molecule, inverse agonist of the receptor is anticipated to reduce production of IL-17, a key pro-inflammatory cytokine. Through a high-throughput screening approach, we identified a molecule displaying promising binding affinity for RORC2, inhibition of IL-17 production in Th17 cells, and selectivity against the related RORA and RORB receptor isoforms. Lead optimization to improve the potency and metabolic stability of this hit focused on two key design strategies, namely, iterative optimization driven by increasing lipophilic efficiency and structure-guided conformational restriction to achieve optimal ground state energetics and maximize receptor residence time. This approach successfully identified 3-cyano-N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)benzamide as a potent and selective RORC2 inverse agoni...
Tetrahedron Letters, 2000
Journal of the American Chemical Society, 2003
European Journal of Organic Chemistry, Dec 1, 1999
In Scheme 4 on page 3278, structures 5a and 5b are incorrectly given. The correct scheme is print... more In Scheme 4 on page 3278, structures 5a and 5b are incorrectly given. The correct scheme is printed below. Scheme 4. (a) Pd/C, H 2 , MeOH; (b) pyridineϪSO 3 , DMSO, Et 3 N, CH 2 Cl 2 ; (c) 9, tBuOK, THF, Ϫ78°C; (d) PtO 2 , H 2 , EtOH; (e) Na/NH 3 , EtOH, Ϫ78°C to room temp.; (f) 10%
Journal of Organic Chemistry, Nov 1, 2001
Regio-and stereoselective palladium-catalyzed reactions of allene-substituted 1,3-dienes 1 in ace... more Regio-and stereoselective palladium-catalyzed reactions of allene-substituted 1,3-dienes 1 in acetic acid at room temperature lead to cyclization with formation of a carbon-carbon bond between the middle carbon of the allene and the terminal carbon of the 1,3-diene. Two different types of reactions, both that constitute 1,4-carboacetoxylations of the 1,3-diene, have been developed. In one of the reactions, Pd(II) catalyzes the oxidation of 1 to bicyclic compounds 2, and in the other, Pd(0) catalyzes the transformation of 1 to bicyclic compounds 3. The products 2 are useful for further synthetic transformations and undergo Diels-Alder reactions with dienophiles to give polycyclic ring systems.
L'invention concerne un compose de formule (I), dans laquelle G est un cycle pyrazole tel que... more L'invention concerne un compose de formule (I), dans laquelle G est un cycle pyrazole tel que defini dans la description et R 4 , R 5 , R 6 et R 7 sont tels que definis dans la description ; ou un de ses esters, amides, solvates ou sels pharmaceutiquement acceptables, y compris un sel d'un tel ester ou amide, et un solvate d'un tel ester, amide ou sel. L'invention concerne egalement l'utilisation de tels composes pour le traitement ou la prophylaxie d'un etat associe avec une maladie ou un trouble associe avec l'activite du recepteur d'estrogene.
ChemSusChem, 2021
By extracting lignin, pulp production can be increased without heavy investments in a new recover... more By extracting lignin, pulp production can be increased without heavy investments in a new recovery boiler, the typical bottleneck of a pulp mill. The extraction is performed by using 0.20 and 0.15 weight equivalents of CO 2 and H 2 SO 4 respectively. Herein, we describe lignin esterification with fatty acids using benign reagents to generate a lignin ester mixable with gas oils. The esterification is accomplished by activating the fatty acid and lignin with acetic anhydride which can be regenerated from the acetic acid recycled in this reaction. The resulting mass balance ratio is fatty acid/lignin/acetic acid (2 : 1 : 0.1). This lignin ester can be hydroprocessed to generate hydrocarbons in gasoline, aviation, and diesel range. A 300-hour continuous production of fuel was accomplished. By recirculating reagents from both the esterification step and applying a water gas shift reaction on off-gases from the hydroprocessing, a favorable overall mass balance is realized.
Lagga socken är ett arkeologiskt intressant område med många fornlämningar från järnåldern. Stran... more Lagga socken är ett arkeologiskt intressant område med många fornlämningar från järnåldern. Strandförskjutningen har förändrat området över tid. Långhundraleden, en viktig forntida vattenled, går genom området och är central för att förstå utvecklingen av området. Området låg i Attundaland men var en gränstrakt till Tiundaland. I Tiundaland ligger Gamla Uppsala som påverkat området. Extra stora gravhögar, så kallade storhögar, är många på en liten yta. Det finns också storhögar som är demolerade, men kan hittas på historiska kartor. Kashögen är en av dessa försvunna högar. Kashögen ligger vid Kasby och förledet i ortnamnet, -Kas, är förknippat med vårdkase och varningseldar som användes för kommunikation och varning ifall fiender var i annalkande.Uppsatsen beskriver Kashögen som att vara den första, den största och den storhög som initierar att de andra storhögarna i området byggs
Selective palladium-catalyzed 1,4-functionalization : allenes and dienes in palladium chemistry a... more Selective palladium-catalyzed 1,4-functionalization : allenes and dienes in palladium chemistry and total syntheses of (+)-pseudoconhydrine and (+)-monomorine I
Journal of medicinal chemistry, Jan 21, 2018
The nuclear hormone receptor RORC2 (also known as RORγt) is a promising target for the treatment ... more The nuclear hormone receptor RORC2 (also known as RORγt) is a promising target for the treatment of autoimmune diseases. A small molecule, inverse agonist of the receptor is anticipated to reduce production of IL-17, a key pro-inflammatory cytokine. Through a high-throughput screening approach, we identified a molecule displaying promising binding affinity for RORC2, inhibition of IL-17 production in Th17 cells, and selectivity against the related RORA and RORB receptor isoforms. Lead optimization to improve the potency and metabolic stability of this hit focused on two key design strategies, namely, iterative optimization driven by increasing lipophilic efficiency and structure-guided conformational restriction to achieve optimal ground state energetics and maximize receptor residence time. This approach successfully identified 3-cyano-N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)benzamide as a potent and selective RORC2 inverse agoni...
Tetrahedron Letters, 2000
Journal of the American Chemical Society, 2003