On November 6, 2003, Arrhenius, Thomas; Cheng, Jie-fei; Huang, Yujin; Nadzan, Alex M. published a patent.Reference of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate The title of the patent was Preparation of azolylhexafluoropropanols and related compounds as liver X receptor (LXR) modulators. And the patent contained the following:
A method for modulation of liver X receptor comprises administration of WC(X)(AY)CF2Z [W = specified (substituted) 5-6 membered (aromatic) heterocyclyl, alkynyl; X = H, CF2Z, CF3; XY forms a double bond when A = O; Y = H; Z = F, Br, Cl, iodo, CF3; A = O, S, imino]. Thus, powd. 4Å mol. sieves, N-(pyridin-4-ylmethyl)-1,3-thiazol-2-amine (preparation given), and hexafluoroacetone trihydrate were heated in PhH at 80° for 24 h to give 1,1,1,3,3,3-hexafluoro-2-[2-[(pyridin-4-ylmethyl)amino]-1,3-thiazol-5-yl]propan-2-ol. The latter was refluxed with isonicotinic anhydride in dioxane at 100° for 2 h to give N-(pyridin-4-ylmethyl)-N-[5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]-1,3-thiazol-2-yl]pyridine-4-carboxamide. This at 10 μM gave 2.49-fold induction of ABCA1 gene in THP-1 cells vs. DMSO controls. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Reference of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate
The Article related to azolylhexafluoropropanol preparation liver x receptor lxr modulator, thiazolylhexafluoropropanol preparation liver x receptor lxr modulator, isoxazolylhexafluoropropanol preparation liver x receptor lxr modulator and other aspects.Reference of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate
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