On September 3, 2009, Vicker, Nigel; Su, Xiangdong; Pradaux-Caggiano, Fabienne; Potter, Barry Victor Lloyd published a patent.Category: alcohols-buliding-blocks The title of the patent was Adamantyl, phenyl, and benzyl ketone derivatives as inhibitors of 11β-hydroxysteroid dehydrogenase type I useful in the treatment of diseases and preparation and pharmaceutical compositions thereof. And the patent contained the following:
Title compounds I and their pharmaceutical compositions are prepared and disclosed as inhibitors of 11β-hydroxysteroid dehydrogenase type I (11β-HSD1) useful in the treatment of diseases. Compounds I [X and Z independently = (un)saturated C1-3 carbon chain; Y = S, SO, SO2, CH=CH, CH2CH2, or O; R1 = 1-adamantyl, 2,4,6-trimethylphenyl, 1-(4-chlorophenyl)C3-6 cycloalkyl, or 2-(4-chlorophenyl)propan-2-yl; R2 = (un)substituted 5- to 6- membered N-containing heteroaryl; with the provision that when R1 = 1-adamantyl and X-Y-Z = CH2S, CH2SO, or CH2SO2, then R2 ≠ 1-methylimidazol-2-yl; or when R1 = 1-adamantyl and X-Y-Z = CH2O, then R2 ≠ 2-methylpyridinyl] are claimed. For example, compound II was prepared via substitution of 2-bromo-1-[1-(4-chlorophenyl)cyclopropyl]ethanone with 2-mercapto-1-methylimidazole. Select I were assayed for 11β-HSD1 inhibition and compound II was found to possess >60% inhibition at 1 μM concentration The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Category: alcohols-buliding-blocks
The Article related to adamantyl ketone derivative preparation 11 beta hydroxysteroid dehydrogenase inhibitor, phenyl ketone derivative preparation 11 beta hsd1 inhibitor, benzyl ketone preparation 11 beta hydroxysteroid dehydrogenase type i and other aspects.Category: alcohols-buliding-blocks
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts