15448-77-8Relevant articles and documents
Mechanistic Definition of Trimethylstannylation of 1,4-Dihalobicycloheptanes: Bridgehead Nucleophilic Substitution Mediated by the Intermediacy of Radicals, Radical Anions, Carbanions, and Propellane
Adcock, William,Gangodawila, Hemakanthi
, p. 6040 - 6047 (1989)
A series of 1,4-dihalobicycloheptanes (2; X=Y=halogens) have been synthesized, characterized, and treated with (trimethylstannyl)lithium (Me3SnLi) in the absence and presence of tert-butylamine (TBA).The product distributions of these reactions have been established by 13C and 119Sn NMR spectroscopy and vapor-phase chromatographic analyses.The results clearly indicate that a polar mechanism involving the formation of a carbanion can compete effectively in these systems against a free-radical chain process (SRN1).The latter mechanism was previously shown to dominate the stannlyation reactions of 1,4-dihalobicyclooctanes (1; X = Y = halogens).Most of the initially formed (4-halo(X)bicyclohept-1-yl)lithium derivatives (2; X = halogen, Y = Li) collapse partially (X = Cl) or completely (X = Br and I) to yield the highly reactive propellane, which serves as a transient intermediate in the stannylation process.Most importantly, the competition between the radical and polar mechanisms in 2 is shown to be dependent not only on the nature of the leaving group (Y = Br or I) but also on the substituent (X = H, F, Cl, Br, or I).Factors governing the partitioning between the two mechanisms are considered.
SUBSTITUTED AMIDE COMPOUNDS USEFUL AS FARNESOID X RECEPTOR MODULATORS
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, (2020/08/28)
Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is: (i) halo, cyano, hydroxyl, NRxRx, C(O)OH, C(O)NH2, C1-6 alkyl substituted with zero to 6 R1a, or P(O)R1cR1c; or (ii) L R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R1a, R1c, R2, R3a, R3b, Rx, L, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
Small Molecule Inhibitors of the JAK Family of Kinases
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, (2018/07/05)
2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
HETEROCYCLIC COMPOUNDS AS PI3K-y INHIBITORS
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Paragraph 1187; 1188, (2018/02/28)
This application relates to compounds of Formula (I): or pharmaceutically acceptable salts or stereoisomers thereof, which are inhibitors of PI3K-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
