On March 1, 1994, Brown, George R.; Mallion, Keith B.; Whittamore, Paul R. O.; Brittain, David R. published a patent.Recommanded Product: 160377-42-4 The title of the patent was Quinuclidine derivatives useful as squalene synthase inhibitors and their preparation. And the patent contained the following:
Compounds of formula I and their pharmaceutically acceptable salts [R1 = H, OH; R2 = H; or R1R2 = bond; X = CH2CH2, CH:CH, CC, CH2O, CH2NH, NHCH2, CH2CO, COCH2, CH2S and SCH2; Ar1 = (un)substituted phenylene; Ar2 = (un)substituted heteroaryl; substituent(s) on Ar1 and Ar2 = halo, OH, (di)(alkyl)amino, NO2, cyano, CO2H, (di)(alkyl)carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, haloalkyl, carboxyalkyl, alkanoylamino; provided that when R1 = OH, X ≠ NHCH2 or SCH2] are inhibitors of squalene synthase, and hence useful in treating hypercholesterolemia and atherosclerosis. Possible antifungal use is also mentioned (no data). Processes for preparing I and pharmaceutical compositions containing them are also described. For example, coupling of 3-ethynyl-3-hydroxyquinuclidine with 2-(4-bromophenyl)pyridine (preparations given) using Pd(PPh3)2Cl2, CuI, and Et3N in DMF at 90°, gave title compound II. At 2.5 μM, II gave about 98% inhibition of squalene synthase in vitro; it also inhibited cholesterol biosynthesis in rats at an ED50 of 8 mg/kg (route unspecified). The experimental process involved the reaction of 5-(4-Bromophenyl)pyrimidine(cas: 160377-42-4).Recommanded Product: 160377-42-4
The Article related to quinuclidine preparation squalene synthase inhibitor, antihypercholesterolemic quinuclidine preparation, antiatherosclerotic quinuclidine preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Recommanded Product: 160377-42-4
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia