170235-18-4Relevant articles and documents
3-HYDROXY-2-PHENYL-6-(PYRAZOL-4-YLMETHYL)PYRIDINE DERIVATIVES AS PDE4D INHIBITORS
-
Paragraph 0097, (2020/11/04)
Provided herein are phosphodiesterase 4D (PDE4D) inhibitors of Formula (I), including methods of using the same. Also provided are methods of treating subjects suffering from conditions associated with aberrant PDE activity, in particular Fragile X syndrome, Alzheimer's disease, memory loss, cognitive dysfunction, autistic spectrum disorder, Parkinson's disease, major depression, bipolar disorder, schizophrenia, multiple sclerosis, traumatic brain injury, or chronic traumatic encephalopathy. Formula (I), wherein, R1 is H, C1-6alkyl, or C1-6haloalkyl; R2 is H, C1-3alkyl, or C1-3haloalkyl; R3 and R4 are each H or D, and at least one of R3 and R4 is D; each R5 is independently halo, CN, OH, NO2, C1-6alkoxy, C1-6haloalkoxy, C1-6alkyl, C1-6haloalkyl, O-C3-6cycloalkyl, C1-6hydroxyalkyl, or SO2C1-3alkyl; X and Y are each independently CR6 or N; each R6 is independently H, C1-3alkyl, or C1-3haloalkyl; and n is 0, 1, 2, 3, or 4.
Total synthesis of dimethyl sulfomycinamate
Kelly, T. Ross,Lang, Fengrui
, p. 4623 - 4633 (2007/10/03)
Dimethyl sulfomycinamate (1), a methanolysis product from the natural antibiotic sulfomycin I, is synthesized in 11 steps. The chemistry of various pyridine, thiazole, and oxazole heterocycles and their coupling reactions under palladium catalysis are examined. The key transformations in the synthesis are the selective palladium-catalyzed coupling reactions on doubly activated pyridine 62 and the condensation reaction between bromo ketone 69 and amide 28 to form the oxazole moiety 76. The first preparation of oxazole triflates is described, as are some of their chemical properties.
