19212-27-2Relevant articles and documents
A new β-keto amide synthesis
Chen, Yanping,Sieburth, Scott McN.
, p. 2191 - 2194 (2002)
In a modification of the Wierenga-Skulnick β-ketoester synthesis, the dianions of malonic acid mono-amides were condensed with acid chlorides. Acidic workup led to decarboxylation and isolation of the corresponding β-keto amides in good-to-excellent yield
5- OR 7-AZAINDAZOLES AS BETA-LACTAMASE INHIBITORS
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Page/Page column 41; 42; 43, (2020/09/19)
The present invention relates to β-lactamase inhibitors having the following general formula (I): wherein R1-R4 and X1-X2 are defined in the specification, pharmaceutical composition thereof, and use thereof for the treatment of a bacterial infection, alone or in combination with β-lactam antibiotics and/or other antibiotics and/or other β-lactamase inhibitors.
Electrophile-Directed Diastereoselective Oxonitrile Alkylations
Chepyshev, Sergiy V.,Pitta, Bhaskar Reddy,Vangala, Saidi Reddy,Lujan-Montelongo, J. Armando,Steward, Omar W.,Fleming, Fraser F.
supporting information, p. 2850 - 2853 (2018/02/09)
Diastereoselective alkylation of prochiral oxonitrile dianions with secondary alkyl halides efficiently installs two contiguous stereogenic centers. The confluence of nucleophilic trajectory and the electrophile chirality causes distinct steric differences that allow efficient discrimination for one of the six possible conformers. Numerous oxonitrile-derived dianions efficiently displace secondary alkyl halides propagating the electrophile chirality to efficiently install two contiguous tertiary centers. The prevalence of chiral, secondary electrophiles makes the interdigitated alkylation of chiral electrophiles a particularly attractive route because the resulting oxonitriles are readily transformed into bioactive heterocycles.
SULFONYLAMINOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
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Page/Page column 98-99, (2016/01/25)
Provided are sulfonylaminopyridine compounds that are inhibitors of ITK kinase, compositions containing these compounds and methods for treating diseases mediated by ITK kinase. In particular, provided are compounds of Formula (I), (II) or (III), stereoisomers, tautomers, solvates, prodrugs or pharmaceutically acceptable salts thereof, where n, R1, R2, R3, R6 and R7 are defined herein, pharmaceutical compositions comprising the compound and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, for example, for treating a disease or condition mediated by ITK kinase in a patient.