138163-08-3Relevant articles and documents
Drastic fluorine effect: Complete reversal of the selectivity in the Au-catalyzed hydroalkoxylation reaction of fluorinated haloalkynes
Cloutier, Mélissa,Mamone, Marius,Paquin, Jean-Fran?ois
supporting information, p. 5969 - 5972 (2020/06/04)
The gold-catalyzed hydration reaction of haloalkynes is highly regioselective producing 2-halomethylketones as the sole products. Herein, we document a drastic fluorine effect where the reaction of 1-halo-3,3-difluoroalkynes as substrates leads to a complete reversal of selectivity and produces 3,3-difluoroesters as the unique products.
THERAPEUTICS TARGETING MUTANT ADENOMATOUS POLYPOSIS COLI (APC) FOR THE TREATMENT OF CANCER
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, (2020/07/04)
The present disclosure reports an extensive medicinal chemistry evaluation of a large collection of Truncating APC-Selective Inhibitor (TASIN) compounds. The compounds were evaluated for activity against a series of colon cancer cell lines with and withou
Highly regioselective gold-catalyzed formal hydration of propargylic: Gem -difluorides
Hamel, Jean-Denys,Hayashi, Tatsuru,Cloutier, Mélissa,Savoie, Paul R.,Thibeault, Olivier,Beaudoin, Meggan,Paquin, Jean-Fran?ois
supporting information, p. 9830 - 9836 (2017/12/08)
Herein, we report a highly regioselective gold-catalyzed formal hydration of propargylic gem-difluorides. Not only does this transformation provide access to versatile fluorinated building blocks that were difficult or hardly possible to access beforehand, but it also represents a rare case of a highly regioselective gold-catalyzed hydroalkoxylation of internal alkynes and puts forward the utility of the difluoromethylene unit as a directing group in catalysis.
Ugi-type reactions of spirocyclic indolenines as a platform for compound library generation
Estévez, Verónica,Kloeters, Laura,Kwietniewska, Natalia,Vicente-García, Esther,Ruijter, Eelco,Orru, Romano V.A.
, p. 376 - 380 (2017/02/10)
A simple and efficient method for the synthesis of highly substituted spiroindoline derivatives is presented. A Fischer indolization is combined with Ugi-type reactions to explore the chemical space concerning this privileged structure. Moreover, spiropip
SULFONAMIDE RETINOIC ACID RECEPTOR-RELATED ORPHAN RECEPTOR MODULATORS AND USES THEREOF
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Paragraph 0244, (2016/02/16)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.
RETINOIC ACID RECEPTOR-RELATED ORPHAN RECEPTOR MODULATORS AND USES THEREOF
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Paragraph 0375, (2015/09/28)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.
7-HYDROXY-SPIROPIPIPERIDINE INDOLINYL ANTAGONISTS OF P2Y1 RECEPTOR
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Paragraph 00158, (2014/02/16)
The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of Ρ2Y1 receptor and may be used as medicaments in the treatment and/or prophylaxis of thromboembolic disorders.
INHIBITORS OF CYTOMEGALOVIRUS
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Page/Page column 20; 21, (2014/05/24)
Compounds of Formula (I) wherein R1, R2, R3A, R3B, Y, Z1 and Z2 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
A facile synthesis of the spiroindoline-based growth hormone secretagogue, MK-677
Qi, Xian Liang,Yang, Er Qun,Zhang, Jun Tao,Wang, Tao,Cao, Xiao Ping
scheme or table, p. 661 - 664 (2012/07/03)
A facile and improved route for the synthesis of the orally active spiroindoline-based growth hormone secretagogue, MK-677 was described. The key step adopted the Fischer indole/reduction strategy. The preparation of the key intermediates N-protected piperidine carboxaldehyde 5 and the N-Boc-O-benzyl-d-serine (2) are also optimized.
Substituted Disulfonamide Compounds
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Page/Page column 31, (2010/06/22)
Substituted disulfonamide compounds corresponding to formula I: In which R1, R2, R3, R4a, R4b, R5a, R5b, R8, R9a, R9b, R10, R11, a, b, s, t and A have defined meanings, pharmaceutical compositions containing one or more such compounds, processes for preparing such compounds, and a method of using such compounds for the treatment or inhibition of pain and/or other conditions mediated by the bradykinin receptor 1 (BR1).