ChemInform Abstract: ON THE SYNTHESIS OF 4‐ AND 5‐PYRIMIDINYLDIPHENYL‐(1‐IMIDAZOLYL)METHANES AND THEIR ANTIFUNGAL ACTIVITY

Abstract

Grignardierung der Pyrimidinylester (I) bzw. (VIa) mit dem Reagenz (II) liefert die Carbinole (III) bzw. (VII), die mit Thionyldiimidazol (IV) zu den Imidazolylmethanen (V) bzw. (VIII) reagieren.

Generic Enhanced Sub/Supercritical Fluid Chromatography: Blueprint for Highly Productive and Sustainable Separation of Primary Hindered Amines

“…Several other compounds contain substructure 1, including structures related to melaninconcentrating hormone receptor (MCHR) antagonists, 2 neuropeptide Y antagonists, 3 human plasma kallikrein inhibitors, 4 β-secretase 1 (BACE1) inhibitors, 5−7 transient receptor potential cation channel subfamily M member 8 (TRPM8) inhibitors, 8,9 cholesteryl ester transfer protein (CETP) inhibitors, 10 and cell division cycle 7 kinase (CDC7) inhibitors 11 relevant to treating cancer; included as well are herbicides 12 and fungicides . 13 In contrast to the breadth of synthetic methods that exist to generate fully substituted carbon centers α to secondary and tertiary amines, 14 access to hindered primary amines is an underdeveloped area. 15 The limitation in synthetic methods to such amines restricts both the access to potentially ground-breaking new molecular entities for pharmaceutical therapies and the options available for developing scalable manufacturing routes to such bioactive compounds.…”

“…Such hindered amines include α,α-diaryl primary amines represented by substructure 1 , which are of interest for the development of bioactive molecules (Figure ). Several other compounds contain substructure 1 , including structures related to melanin-concentrating hormone receptor (MCHR) antagonists, neuropeptide Y antagonists, human plasma kallikrein inhibitors, β-secretase 1 (BACE1) inhibitors, − transient receptor potential cation channel subfamily M member 8 (TRPM8) inhibitors, , cholesteryl ester transfer protein (CETP) inhibitors, and cell division cycle 7 kinase (CDC7) inhibitors relevant to treating cancer; included as well are herbicides and fungicides . In contrast to the breadth of synthetic methods that exist to generate fully substituted carbon centers α to secondary and tertiary amines, access to hindered primary amines is an underdeveloped area .…”