119736-09-3Relevant articles and documents
Direct Palladium-Catalyzed β-Arylation of Lactams
Chen, Ming,Liu, Feipeng,Dong, Guangbin
supporting information, p. 3815 - 3819 (2018/03/13)
A direct and catalytic method is reported here for β-arylation of N-protected lactams with simple aryl iodides. The transformation is enabled by merging soft enolization of lactams, palladium-catalyzed desaturation, Ar?X bond activation, and aryl conjugate addition. The reaction is operated under mild reaction conditions, is scalable, and is chemoselective. Application of this method to concise syntheses of pharmaceutically relevant compounds is demonstrated.
RORγ MODULATORS
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Page/Page column 29, (2015/04/15)
Described are RORγ modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The invention includes stereoisomeric forms of the compounds of formula I, including stereoisomerically-pure, scalemic and racemic form, as well as tautomers thereof. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
Antibiotic sulfonylaminocarbonyl activated beta-lactams
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, (2008/06/13)
This invention presents novel 2-azetidinone compounds which are useful as antibacterial agents to eradicate or control susceptible microbes of the formula STR1 wherein R401 and R402 are the same or different and are (a) hydrogen, (b) (C1 -C12) alkyl (c) (C2 -C8) alkenyl, (d) (C2 -C8) alkynyl, (e) (C3 -C10) cycloalkyl, (f) phenyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C1 -C4) alkyl, and (C1 -C4) alkoxy, (g) benzyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C1 -C4) alkyl, and (C1 -C4) alkoxy, (h) --CH2 --O--CO--CH2 --NHR420, (i) --CH2 --O--CO2 --R430, (j) --CH2 F, or (k) --CHF2 ; wherein R420 is (a) hydrogen, (b) --COH, or (c) --CO--O--C(CH3)3 ; wherein R430 is (C1 -C8) alkyl, --(CH2) 2 OC(O)NH2, --(CH 2)2 Cl, --(CH2)2 OCH3 or --(CH2)2 NHCOH; wherein R300 is an acyl group derived from a carboxylic acid; wherein R100 is an optionally substituted heterocyclic moiety of Formula 2, 3, 4 or 5 STR2