660862-47-5Relevant articles and documents
KRAS G12C INHIBITORS
-
, (2021/06/22)
The present invention provides compounds of the formula: where R1, R2, R3, R4, R5, A, B, and Y are as described herein, pharmaceutically acceptable salts thereof, and methods of using these compounds and salts for treating patients for cancer.
COMBINATION OF HEPATITIS B VIRUS (HBV) VACCINES AND DIHYDROPYRIMIDINE DERIVATIVES AS CAPSID ASSEMBLY MODULATORS
-
Page/Page column 119-120, (2021/01/22)
Therapeutic combinations of hepatitis B virus (HBV) vaccines and capsid assembly modulators (CAMs), such as dihydropyrimidine derivatives are described. Methods of inducing an immune response against HBV or treating an HBV-induced disease, particularly in individuals having chronic HBV infection, using the disclosed therapeutic combinations are also described.
Synthesis of a bicyclic piperazine from l-aspartic acid and application of a fluoride-promoted SNAr coupling
Sieser, Janice E.,Singer, Robert A.,McKinley, Jason D.,Bourassa, Dennis E.,Teixeira, John J.,Long, James
, p. 1328 - 1335 (2012/01/12)
The process development is reported of a pivotal C-N bond formation involving ((7R,9aS)-octahydro-1H-pyrido[1,2-a]pyrazin-7-yl)methanol (2) undergoing nucleophilic aromatic substitution with 3-chlorobenzo[d]isoxazole (3) to furnish ((7R,9aS)-2-(benzo[d]isoxazol-3-yl)octahydro-1H-pyrido[1,2-a] pyrazin-7-yl)methanol (4) as a key intermediate for a family of compounds (1). Essential to the success of the coupling is the use of fluoride in combination with a phase transfer catalyst. The development of an alternative route to bicyclic piperazine 2 that uses l-aspartic acid (20) as a starting material to avoid the need for a classical salt resolution is described.