121659-86-7

Usage

Chemical Properties

White Solid

Uses

Pitavastatin intermediate.

Upstream product

• 449181-32-2 4-Fluoro-2'-aminobenzophenone methansulfonic acid salt 
• 32249-35-7 methyl 3-cyclopropyl-3-oxopropanoate 
• 765-43-5 Cyclopropyl methyl ketone 
• 1765-93-1 4-fluoroboronic acid 
• 3800-06-4 2-amino-4'-fluorobenzophenone 
• 462-06-6 fluorobenzene 
• 552-16-9 ortho-nitrobenzoic acid 
• 120303-62-0 (4-fluorophenyl)(2-nitrophenyl)methanone 

Downstream Products

• 154057-58-6 <2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl>methyltriphenylphosphonium bromide 
• 147526-32-7 pitavastatin calcium salt 
• 147526-32-7 pitavastatin 
• 574705-92-3 sodium (3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoate 
• 147489-06-3 (4R,6S)-(E)-{6-[2-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-vinyl]-2,2-dimethyl-1,3-dioxan-4-yl}acetic acid tert-butyl ester 
• 586966-54-3 (3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-3,5-dihydroxy-6-heptenoic acid tert-butyl ester 
• 172336-32-2 ethyl (E)-3,5-dihydroxy-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]hept-6-enoate 
• 391681-95-1 2-cyclopropyl-3-(3-ethoxy-1-hydroxy-2-propenyl)-4-(4-fluorophenyl)quinoline 
• 172336-32-2 (±)-E-3,5-dihydroxy-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-6-heptenoic acid ethyl ester 
• 148901-69-3 (E)-7-[2-cyclopropyl-4-(4-fluorophenyl)-quinolin-3-yl]-5-hydroxy-3-oxohept-6-enic acid ethyl ester 
• 148901-68-2 (E)-3-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-propenal 
• 121660-37-5 2-cyclopropyl-4-(4-fluorophenyl)-3-formylquinoline 
• 121660-11-5 2-cyclopropyl-4-(4-fluorophenyl)-3-(hydroxymethyl)quinoline 

Relevant academic research and scientific papers

Preparation method of intermediate of pitavastatin calcium

The invention relates to a preparation method of an intermediate 2-cyclopropyl-4-(4-fluorophenyl)-3-quinolinecarboxylate of pitavastatin calcium. The method comprises the following steps: with 2-aminobenzonitrile and 3-cyclopropyl-3-oxo-propionate as star

Palladium-Catalyzed Carbonylative Couplings of Vinylogous Enolates: Application to Statin Structures

The first Pd-catalyzed carbonylative couplings of aryl and vinyl halides with vinylogous enolates are reported generating products derived from C-C bond formation exclusively at the γ-position. Good results were obtained with a dienolate derivative of acetoacetate (1,3-dioxin-4-one). These transformations occurred at room temperature and importantly with only stoichiometric carbon monoxide in a two-chamber reactor. The methodology was applied to the synthesis of two members of the statin family generating the cis-3,5-diol acid motif by a γ-selective carbonylation followed by a cis-stereoselective reduction of the 3,5-dicarbonyl acid intermediates.

Process for Preparing Pitavastatin, Intermediates and Pharmaceuctically Acceptable Salts Thereof

Processes for preparing pravastatin, intermediates and pharmaceutically acceptable salts thereof are provided Crystalline forms of pravastatin, intermediates and pharmaceutically acceptable salts thereof are also disclosed.

PROCESS FOR PRODUCING QUINOLINE-3-CARBOXYLIC ACID COMPOUND

A process for producing quinoline-3-carboxylic acid represented by formula (3) wherein R1, R2, R3, R4 and R5 have the same meanings as defined below, characterized by reacting 2-aminophenyl ketone rep

Synthesis and biological evaluations of quinoline-based HMG-CoA reductase inhibitors

A series of quinoline-based 3,5-dihydroxyheptenoic acid derivatives were synthesized from quinolinecarboxylic acid esters by homologation, aldol condensation with ethyl acetoacetate dianion, and reduction of 3-hydroxyketone to evaluate their ability to inhibit the enzyme HMG-CoA reductase in vitro. In agreement with previous literature, a strict structural requirement exists on the external ring, and 4-fluorophenyl is the most active in this system. For the central ring, substitution on positions 6, 7, and 8 of the central quinoline nucleus moderately affected the potency, whereas the alkyl side chain on the 2-position had a more pronounced influence on activity. Among the derivatives, NK-104 (pitavastatin calcium), which has a cyclopropyl group as the alkyl side chain, showed the greatest potency. We found that further modulation and improvement in potency at inhibiting HMG-CoA reductase was obtained by having the optimal substituents flanking the desmethylmevalonic acid portion, that is, 4-fluorophenyl and cyclopropyl, instead of the usual isopropyl group.