A Facile Synthesis of 2-Aminonicotinaldehyde

Direct Synthesis of Imines from gem-Dibromomethylaryl Derivatives: Application to Unsymmetrically Substituted Bipyridine Frameworks

“…Examples for the preparation of an imino compound from molecules where the aldehyde function is masked in the form of a gem -dibromomethyl derivative appeared to be rare and not specifically designed for preparative purposes . However, in some cases, the intermediate imino derivative is postulated to undergo an intramolecular rearrangement, leading to substituted heterocycles such as pyrazines, benzopyrazines, triazines, benzimidazoles, and elaborated poly-heteroaromatic derivatives .…”

Discovery of Diphenylmethanepropionic and Dihydrostilbeneacetic Acids as Antagonists of the Integrin αvβ3

“…This compound was synthesized starting from 1‐tetralone through the phenolic intermediate 31 as shown in Scheme 4. At this point we also had optimized the guanidine surrogate part of the molecule and found tetrahydro‐1,8‐naphthyridine‐2‐ethanol (27–30) to be superior to aminopyridine moiety in potency. Mitsunobu coupling of 32 with phenol 31 followed by saponification afforded the desired product 7 .…”