- Benzonorbornadiene Derivatives and Reactions Thereof
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A bioorthogonal molecule can include a molecule having a structure according the above wherein R1-R8 are independently selected from H, a substituted or unsubstituted C1-C4 alkyl or alkylene group, COOH, COORsu
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Paragraph 0311-0312
(2019/10/17)
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- Rapid and efficient tetrazine-induced drug release from highly stable benzonorbornadiene derivatives
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A novel class of bioorthogonal release reactions based on benzonorbornadiene derivatives was developed. These carrier molecules are highly stable at physiological conditions, but react rapidly with 1,2,4,5-tetrazines, and near-quantitatively release cargo
- Xu, Minghao,Tu, Julian,Franzini, Raphael M.
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supporting information
p. 6271 - 6274
(2017/07/10)
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- Palladium-catalyzed regioselective allylation of five-membered heteroarenes with allyltributylstannane
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Palladium-catalyzed allylation reactions of 2-(chloromethyl)thiophenes, 2-(chloromethyl)furans, and N-protected 2-(chloromethyl)-1H-pyrroles with allyltributylstannane were described in this study. This type of allylation reaction regioselectively occurred on the heteroarene rings to produce allylated dearomatization products or allylated heteroarenes with satisfactory yields.
- Zhang, Sheng,Yu, Xiaoqiang,Feng, Xiujuan,Yamamoto, Yoshinori,Bao, Ming
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p. 3842 - 3845
(2015/03/30)
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- 4-PHENYL-5-OXO-1,4,5,6,7,8-HEXAHYDROQUINOLINE DERIVATIVES THE TREATMENT OF INFERTILITY
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The present invention relates to 4-phenyl-5-oxo-l,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein R1 is (l-6C)alkyl, (2-6C)alkenyl or (2-6C)aDcynyl; R2, R3 are independently halogen, (l-4C)allcyl, (2-4C)alkenyl, (2-4C)- alkynyl, (1 -4C)aBcoxy, (3-4C)alkenyloxy or (3-4C)alkynyloxy; R4 is phenyl or (2-5C)- heteroaryl, both substituted with R7 and optionally substituted on the (hetero)aromatic ring with one or more substituents selected from hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (l-4C)alkyl, (l-4C)alkoxy , (l-4C)alkylthio and (di)(l-4C)- alkylamino. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 4-phenyl-5-oxo-l, 4,5,6, 7,8-hexahydro- quinoline derivatives in therapy, more specifically for the treatment of infertility
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Page/Page column 63
(2010/11/24)
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- INHIBITORS OF DIPEPTIDYLPEPTIDASE IV
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The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods of using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor that contain a carboxylic acid moiety. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.
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Page/Page column 69
(2008/06/13)
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- Synthesis and properties of ring-deactivated deuterated (hydroxymethyl)pyrroles
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A sequence, based on a Mitsunobu displacement at the hydroxymethyl position of deuterium-labeled, N-substituted 2-(hydroxymethyl)pyrroles, is reported as a general procedure to determine the ability of the N-substituent to deactivate the heterocycle. An S
- Abell, Andrew D.,Nabbs, Brent K.,Battersby, Alan R.
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p. 1741 - 1746
(2007/10/03)
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- Synthesis of pyranose glycals via tungsten and molybdenum pentacarbonyl-induced alkynol cyclizations
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The tungsten pentacarbonyl-induced cyclization of an acyclic alkynol substrate bearing protected oxygen and nitrogen functional groups provides the cyclic tungsten oxacarbene, which is readily converted into a pyranose glycal structurally related to the carbohydrate moieties of the pluramycin and vancomycin families of antitumor antibiotics. In addition a molybdenum-catalyzed cycloisomerization procedure provides an alternative route to this pyranose glycal.
- McDonald, Frank E.,Zhu, Hugh Y. H.
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p. 11061 - 11068
(2007/10/03)
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- Synthesis of N-protected 2-hydroxymethylpyrroles and transformation into acyclic oligomers
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The synthesis of N-tosylated and N-Boc-protected 2-hydroxymethyl-pyrroles 2a-c and 3a-d and their transformation into di- and tripyrroles 18, 20a and 20b as well as the preparation of the vinyl- and ethynylpyrroles 13a, 13b and 15 is described. The pyrrole-2-carboxylic acid ethyl esters 7a and b and the pyrrole-2-carbaldehydes 4a-d were transformed into their N-protected derivatives 5a, 5b, 6a-d, 8a and 8b in 69-97% yield and reduced to give the corresponding hydroxymethylpyrroles 2a-c and 3a-d in 79-96% yield; treatment of 2b with 17, 19a and 19b in 0.5% hydrochloric acid gives the dipyrrole 18 and the tripyrroles 20a and 20b in 20-28% yield.
- Tietze, Lutz F.,Kettschau, Georg,Heitmann, Katja
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p. 851 - 857
(2007/10/03)
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- Divergent pathways in the intramolecular reactions between rhodium-stabilized vinylcarbenoids and pyrroles: Construction of fused tropanes and 7-azabicyclo[4.2.0]octadienes
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The rhodium(II)-catalyzed intramolecular reaction between vinyldiazomethanes and pyrroles leads to a novel synthesis of fused tropanes. The reaction occurs by a stepwse 3 + 4 annulation mechanism between a rhodium-stabilized vinylcarbenoid intermediate and the pyrrole rather than by the typical tandem cyclopropanation/Cope rearrangement sequence. The outcome of the reaction is very sensitive to the vinylcarbenoid structure. In particular, the presence of a 2-siloxy substituent on the vinylcarbenoid strongly favors the formation of fused tropanes. In the absence of such functionality, the formation of fused 7-azabicyclo[4.2.0]octadienes becomes the dominant reaction pathway.
- Davies, Huw M. L.,Matasi, Julius J.,Ahmed, Gulzar
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p. 2305 - 2313
(2007/10/03)
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