- IMINO SULFANONE INHIBITORS OF ENPP1
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The present disclosure relates generally to inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions thereof, and methods of using said compounds and compositions thereof. More specifically, the present disclosure relates to sulfoximine- based inhibitors of ENPP1 of Formula (I) and methods of their use for treating disease mediated by ENPP1.
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Paragraph 0184
(2021/11/13)
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- Synthesis of 4-alkylidene-4H-3,1-benzoxazine derivatives by acid-catalyzed cyclization of 2-isocyanophenyl ketones in the presence of a vinyl ether
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2-(1-Alkoxyalkyl)-4-alkylidene-4H-3,1-benzoxazines are conveniently prepared by the reaction of 1-(2-isocyanophenyl) ethanones or 1-(2-isocyanophenyl)propan-1-ones with a vinyl ether, such as 2-methoxypropene or ethyl vinyl ether, in the presence of a catalytic amount of (±)-camphor-10-sulfonic acid. Georg Thieme Verlag Stuttgart.
- Kobayashi, Kazuhiro,Okamura, Yuta,Konishi, Hisatoshi
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experimental part
p. 1494 - 1498
(2009/12/06)
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- Simple route to 3-(2-indolyl)-1-propanones via a furan recyclization reaction
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A simple route to 1-R-3-(2-indolyl)-1-propanones has been elaborated based on recyclization of 2-(2-aminobenzyl)furan derivatives. Being a modification of the Reissert indole synthesis, our approach employs the furan ring as a source of carbonyl function. This approach is general and allows varying of substituents in aromatic ring as well as in 3-position of indole nucleus.
- Butin, Alexander V.,Smirnov, Sergey K.,Stroganova, Tatyana A.,Bender, Wolfgang,Krapivin, Gennady D.
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p. 474 - 491
(2007/10/03)
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- Synthesis and antitumor activity of 20(S)-camptothecin derivatives. A-ring-substituted 7-ethylcamptothecins and their E-ring-modified water-soluble derivatives
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Twenty-six novel A-ring-modified 7-ethylcamptothecins (6) were synthesized by Friedlander's condensation of the chiral tricyclic ketone (5) with aminopropiophenones (4). The compounds substituted with fluorine at the 11 position showed strong cytotoxicity
- Yaegashi,Sawada,Nagata,Furuta,Yokokura,Miyasaka
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p. 2518 - 2525
(2007/10/02)
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- Camptothecin derivatives
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New campotothecin derivatives and a process for preparing same are disclosed, which are represented by the general formula: STR1 wherein R1 represents a lower alkyl group, R2 represents a hydrogen atom or an amino, hydroxyl, lower acylamino or lower alkoxy group, R3 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, nitro, amino, cyano or di(lower alkyl)amino group, R4 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, lower alkylthio, amino, cyano or di(lower alkyl)amino group, and R5 represents a hydrogen or halogen atom or a hydroxyl or lower alkoxy group, with the proviso that all of the R2, R3, R4 and R5 substituents should not be a hydrogen atom and also that if any one of the R2, R3, R4 and R5 is a hydroxyl or lower alkoxy group, all of the other three substituents should not be a hydrogen atom.
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