867308-96-1

Basic information

• Product Name: 1-[2-((4R,6R)-6-tert-Butoxycarbonylmethyl-2,2-dimethyl-[1,3]dioxan-4-yl)-ethyl]-2-(4-fluoro-phenyl)-5-cyclopropyl-1H-imidazole-4-carboxylic acid benzyl ester
• Synonyms: 1-[2-((4R,6R)-6-tert-Butoxycarbonylmethyl-2,2-dimethyl-[1,3]dioxan-4-yl)-ethyl]-2-(4-fluoro-phenyl)-5-cyclopropyl-1H-imidazole-4-carboxylic acid benzyl ester
• CAS NO: 867308-96-1
• Molecular Weight: 592.708
• Mol File: 867308-96-1.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: 1-[2-((4R,6R)-6-tert-Butoxycarbonylmethyl-2,2-dimethyl-[1,3]dioxan-4-yl)-ethyl]-2-(4-fluoro-phenyl)-5-cyclopropyl-1H-imidazole-4-carboxylic acid benzyl ester(CAS DataBase Reference)
• NIST Chemistry Reference: 1-[2-((4R,6R)-6-tert-Butoxycarbonylmethyl-2,2-dimethyl-[1,3]dioxan-4-yl)-ethyl]-2-(4-fluoro-phenyl)-5-cyclopropyl-1H-imidazole-4-carboxylic acid benzyl ester(867308-96-1)
• EPA Substance Registry System: 1-[2-((4R,6R)-6-tert-Butoxycarbonylmethyl-2,2-dimethyl-[1,3]dioxan-4-yl)-ethyl]-2-(4-fluoro-phenyl)-5-cyclopropyl-1H-imidazole-4-carboxylic acid benzyl ester(867308-96-1)

Safety Data

• Hazardous Substances Data: 867308-96-1(Hazardous Substances Data)

Upstream product

• 2462-31-9 benzyl 2-aminoacetate hydrochloride 
• 81477-91-0 benzyl 2-(diphenylmethyleneamino)acetate 
• 1319747-57-3 C₂₆H₂₃NO₃ 
• 867308-95-0 3-Cyclopropyl-2-(4-fluoro-benzoylamino)-3-oxo-propionic acid benzyl ester 
• 125971-86-0 tert-butyl [(4R,6R)-6-aminoethyl-2,2-dimethyl-1,3-dioxan-4-yl]acetate 

Downstream Products

• 867305-04-2 1-[2-((4R,6R)-6-tert-Butoxycarbonylmethyl-2,2-dimethyl-[1,3]dioxan-4-yl)-ethyl]-5-cyclopropyl-2-(4-fluoro-phenyl)-1H-imidazole-4-carboxylic acid 
• 1309777-86-3 C₂₈H₃₁FN₃O₆^(1-)*Na⁽¹⁺⁾ 
• 1309777-87-4 C₂₈H₃₁FN₃O₆^(1-)*Na⁽¹⁺⁾ 
• 1309777-88-5 C₂₇H₂₈F₂N₃O₅^(1-)*Na⁽¹⁺⁾ 
• 1309777-89-6 (3R,5R)-7-(4-((3-fluorobenzyl)carbamoyl)-5-cyclopropyl-2-(4-fluorophenyl)-1H-imidazol-1-yl)-3,5-dihydroxyheptanoic acid 
• 1309777-90-9 C₂₇H₂₈F₂N₃O₅^(1-)*Na⁽¹⁺⁾ 
• 1309777-91-0 C₂₇H₂₇F₃N₃O₅^(1-)*Na⁽¹⁺⁾ 
• 1309777-92-1 C₂₇H₂₇F₃N₃O₅^(1-)*Na⁽¹⁺⁾ 
• 1309777-93-2 C₂₈H₃₀F₂N₃O₅^(1-)*Na⁽¹⁺⁾ 
• 1309777-94-3 C₂₈H₃₀F₂N₃O₆^(1-)*Na⁽¹⁺⁾ 
• 1309777-95-4 C₂₈H₃₀FN₄O₆^(1-)*Na⁽¹⁺⁾ 
• 1309777-96-5 C₂₉H₃₄FN₄O₇S^(1-)*Na⁽¹⁺⁾ 
• 1319751-45-5 C₃₄H₄₂FN₃O₅ 
• 1319751-46-6 C₃₅H₄₄FN₃O₅ 

Relevant articles and documents

Discovery of novel hepatoselective HMG-CoA reductase inhibitors for treating hypercholesterolemia: A bench-to-bedside case study on tissue selective drug distribution

The design of drugs with selective tissue distribution can be an effective strategy for enhancing efficacy and safety, but understanding the translation of preclinical tissue distribution data to the clinic remains an important challenge. As part of a discovery program to identify next generation liver selective HMG-CoA reductase inhibitors we report the identification of (3R,5R)-7-(4-((3-fluorobenzyl)carbamoyl)-5-cyclopropyl-2-(4-fluorophenyl) -1H-imidazol-1-yl)-3,5-dihydroxyheptanoic acid (26) as a candidate for treating hypercholesterlemia. Clinical evaluation of 26 (PF-03491165), as well as the previously reported 2 (PF-03052334), provided an opportunity for a case study comparison of the preclinical and clinical pharmacokinetics as well as pharmacodynamics of tissue targeted HMG-CoA reductase inhibitors.

Novel imidazoles

Novel imidazoles are provided. The compounds are useful as HMGCo-A Reductase Inhibitor. Also provided are pharmaceutical compositions of the compounds. Methods of making and methods of using the compounds are also provided.