163089-34-7Relevant academic research and scientific papers
1,2,3-BENZOTRIAZOLE DERIVATIVES AS ROR GAMMA T MODULATORS
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Page/Page column 57, (2018/03/25)
The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, G, L, R1, Rx, Ry, X1, X2, X3, X4, n, p, q and t are
SERINE/THREONINE KINASE INHIBITORS
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Paragraph 00268, (2013/09/12)
Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
5,7-SUBSTITUTED-IMIDAZO[1,2-C]PYRIMIDINES
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Paragraph 00379, (2013/04/25)
Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
SERINE/THREONINE KINASE INHIBITORS
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Page/Page column 135, (2012/09/21)
Compounds having the formula I wherein Z, Z1 Z2 Z3, R3a, R3b and Rb and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperprolife
The rhodium-catalyzed carbene cyclization cycloaddition cascade reaction of vinylsulfonates
Shi, Bairu,Merten, Sandra,Wong, David K. Y.,Chu, John C. K.,Liu, Lok Lok,Lam, Sze Kui,J?ger, Anne,Wong, Wing-Tak,Chiu, Pauline,Metz, Peter
supporting information; experimental part, p. 3128 - 3132 (2010/04/24)
Vinylsulfonates have proved to be excellent dipolarophiles for carbonyl ylides derived from diazoketones in rhodium-catalyzed intramolecular cycloadditions. Polyfunctional substrates, such as 8 and (+)-15, were readily available from hydroxy esters, e.g. 1 and the cyclopenta-1,3-dione 10, respectively, and the resulting polycyclic sultones were formed under mild reaction conditions in high yields with very good diastereoselectivities. A ruthenium-catalyzed asymmetric transfer hydrogenation was found to desymmetrize the meso-cyclopenta-1,3-dione 12 efficiently.
Efficient synthesis of 4′-cyclopropylated carbovir analogues with use of ring-closing metathesis from glycolate
Liu, Lian Jin,Yoo, Jin Cheol,Hong, Joon Hee
experimental part, p. 1186 - 1196 (2009/04/11)
The first synthetic route of novel 4′-cyclopropylated carbovir analgues is described. The construction of cyclopropylated quaternary carbon at 4′-position of carbocyclic nucleosides was successfully made via sequential Johnson's orthoester rearrangement and ring-closing metathesis (RCM) starting from ethyl glycolate. Synthesized compounds 15 and 16 showed moderate antiviral activity without any cytotoxicity up to 100 μmol. Copyright Taylor & Francis Group, LLC.
Enantioselective synthesis of α-tertiary hydroxyaldehydes by palladium-catalyzed asymmetric allylic alkylation of enolates
Trost, Barry M.,Xu, Jiayi,Reichle, Markus
, p. 282 - 283 (2007/10/03)
Chiral α-tertiary hydroxyaldehydes are very versatile building blocks in synthetic chemistry. Herein, we report the first examples of a catalytic asymmetric protocol for the synthesis of such compounds from readily available α-halo or α-hydroxy ketones or enol silyl ethers with excellent yields and enantioselectivity. Its synthetic utility is demonstrated in the short, efficient formal synthesis of (S)-oxybutynin. In this process, the chiral ligand controls the regioselectivity as well as the enantioselectivity. Copyright
Concise synthesis of the neo-clerodane skeleton of teucrolivin A using a pericyclic reaction cascade
Arns, Steve,Barriault, Louis
, p. 1809 - 1816 (2007/10/03)
Herein, we describe the synthesis of advanced intermediate 39 on the path towards the total synthesis of teucrolivin A (3) in 16 steps from commercially available 1,3-cyclohexadiene. We have constructed the trans-decalin core of the natural product 3 as a
Complex aldol reactions for the construction of dense polyol stereoarrays: Synthesis of the C33-C36 region of aflastatin A
Evans, David A.,Glorius, Frank,Burch, Jason D.
, p. 3331 - 3333 (2007/10/03)
(Chemical Equation Presented) Facial selectivity in the addition of boron enolates of α-oxygenated ketones to anti-disposed α,β-bisalkoxy aldehydes is controlled by the aldehyde vicinal diol protecting group. Protection of the diol as an acetonide results in the exclusive formation of the anti-syn-anti stereoarray found in the C33-C36 region of aflastatin A.
