- PYRAZOLOCHLOROPHENYL COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF
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Compounds of Formula (I) and methods of use as Janus kinase inhibitors are described herein.
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- Synthesis of 4-Quinolones: N,O-Bis(trimethylsilyl)acetamide-Mediated Cyclization with Cleavage of Aromatic C-O Bond
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The synthesis of 1,4-dihydro-4-oxoquinoline derivatives (4-quinolones) based on a BSA [N,O-bis(trimethylsilyl)acetamide]-mediated cyclization of substituted 1-(2-methoxyphenyl)-3-(alkyl/arylamino)prop-2-en-1-ones is described. The reaction belongs to a rare set of cyclizations in which a methoxy group serves as the leaving group. Reaction takes place by the action of silylating agent under mild conditions and provides high yields of pure products following simple aqueous work-up. The versatility of the approach is exemplified by a wide range of 1-alkyl/aryl 3-carboxylates and 3-nitriles that have been prepared. A crucial advantage of this approach is the facile availability of starting methoxy compounds enabling new synthetic possibilities as well as improved cost efficiency. A new approach to the synthesis of 1,4-dihydro-4-oxoquinoline (4-quinolone) derivatives using a BSA-mediated reaction was developed; this entails an example of rare cyclizations in which an OMe group serves as a leaving group. This transformation has great synthetic potential due to the phenolic framework of starting materials and the mildness of the reagent.
- Pí?a, Ond?ej,Rádl, Stanislav
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p. 2336 - 2350
(2016/05/19)
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- PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS
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A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical
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