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99% Purity Commercial production Pitavastatin 147511-69-1 with Cheapest Price
- Molecular Formula:C25H24FNO4
- Molecular Weight:421.468
- Vapor Pressure:4.21E-20mmHg at 25°C
- Refractive Index:1.679
- Boiling Point:691.961 °C at 760 mmHg
- PKA:4.24±0.10(Predicted)
- Flash Point:372.285 °C
- PSA：90.65000
- Density:1.352 g/cm3
- LogP:4.51810
Pitavastatin(Cas 147511-69-1) Usage
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Reference |
https://en.wikipedia.org/wiki/Pitavastatin http://www.rxlist.com/livalo-drug.htm https://www.drugs.com/cdi/pitavastatin.html |
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Biological Activity |
pitavastatin (nk-104) is a potent hmg-coa reductase inhibitor, pitavastatin inhibited cholesterol synthesis from acetic acid with an ic50 of 5.8 nm in a human liver cancer cell line (hepg2). |
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Enzyme inhibitor |
This HMG-CoA reductase inhibitor (FW = 421.46 g/mol; CAS 147511-69- 1; IUPAC Name: (3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin- 3-yl]-3,5-dihydroxyhept-6-enoic acid), also known as itavastatin, itabavastin, nisvastatin, NK-104, NKS-104, and the trade name Livalo?, is indicated for ameliorating hypercholesterolemia and preventing cardiovascular disease. NK-104 potency is dose-dependent and is roughly equivalent to that of atorvastatin. It is well-tolerated in the treatment of patients with hypercholesterolemia. Pitavastatin uptake is carrier-mediated. Target(s): Reduces inflammatory cytokine production from human bronchial epithelial cells; Decreases microtubule tau protein levels via the inactivation of Rho/ROCK; Inhibits hepatic steatosis and fibrosis in non-alcoholic steatohepatitis model; Suppresses therosclerosis induced by chronic inhibition of the synthesis of nitric oxide in moderately hypercholesterolemic rabbits; Decreases the expression of endothelial lipase both in vitro and in vivo; Inhibits NFkB pathway in brain; Inactivates NFkB and decreases IL-6 production through Rho kinase pathway in MCF-7 human breast cancer cells; Reduces C-reactive-protein-induced interleukin-8 production in human aortic endothelial cells; Inhibits lysophosphatidic acid-induced proliferation and monocyte chemoattractant protein-1 expression in aortic smooth muscle cells by suppressing Rac-1-mediated reactive oxygen species generation; Inhibits upregulation of intermediate conductance calcium-activated potassium channels and coronary arteriolar remodeling induced by long-term blockade of nitric oxide synthesis; Inhibits migration and proliferation of rat vascular smooth muscle cells. |
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Definition |
ChEBI: A hydroxy monocarboxylic acid anion that is the conjugate base of pitavastatin, obtained by deprotonation of the carboxy group. |
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Brand name |
[Name previously used: Itavastatin]. |
InChI:InChI=1/C25H24FNO4/c26-17-9-7-15(8-10-17)24-20-3-1-2-4-22(20)27-25(16-5-6-16)21(24)12-11-18(28)13-19(29)14-23(30)31/h1-4,7-12,16,18-19,28-29H,5-6,13-14H2,(H,30,31)/b12-11+
147511-69-1 Relevant articles
Method for preparing rosuvastatin and pitavastatin 2, 5-diene heptanoate compound
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Paragraph 0031-0033, (2020/05/14)
The invention discloses a method for pre...
Multi-substituted dihydroisoquinolines he the sandbank contains the fluorine derivative and use thereof
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Paragraph 0135; 0136, (2018/06/04)
The invention belongs to the field of ph...
For production of the precursor [...]
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, (2018/03/23)
PROBLEM TO BE SOLVED: To provide a precu...
Method for preparing pitavastatin lactone impurity
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Paragraph 0007, (2016/11/17)
The invention discloses a method for pre...
147511-69-1 Process route
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147526-32-7
pitavastatin calcium salt
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147526-32-7,147511-69-1,688735-41-3,769908-13-6,121659-03-8
pitavastatin
| Conditions | Yield |
|---|---|
|
With
hydrogenchloride;
In
water; ethyl acetate;
at 25 - 35 ℃;
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95.9% |
|
With
hydrogenchloride;
In
dichloromethane; water;
at 0 - 25 ℃;
for 0.833333h;
pH=3;
|
|
|
With
hydrogenchloride;
In
water; ethyl acetate;
pH=4;
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3.7 g |
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With
hydrogenchloride;
In
dichloromethane; water;
|
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![(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](/upload/2026/6/40ee3cae753b4680b32056cb78891916_2b63ba3c-25da-4b29-91a7-0482cf964691.png)
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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
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147526-32-7,147511-69-1,688735-41-3,769908-13-6,121659-03-8
pitavastatin
| Conditions | Yield |
|---|---|
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(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;
With
trifluoroacetic acid;
In
acetonitrile;
at 30 - 35 ℃;
With
caesium carbonate;
In
acetonitrile;
at 35 - 40 ℃;
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94% |
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Multi-step reaction with 3 steps
1.1: water; oxalic acid / methanol / 6 h / 35 °C
1.2: 2.75 h / 10 - 30 °C / pH 7
2.1: sodium hydroxide; water / methanol / 1.67 h / 0 °C
2.2: 0.67 h / 25 °C
3.1: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
With
hydrogenchloride; water; oxalic acid; sodium hydroxide;
In
methanol; dichloromethane; water;
|
|
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Multi-step reaction with 4 steps
1.1: water; oxalic acid / methanol / 6 h / 35 °C
1.2: 2.75 h / 10 - 30 °C / pH 7
2.1: sodium hydroxide; water / acetonitrile / 1.5 h / 30 °C
2.2: 0.25 h / 0 °C / pH 4
2.3: 0.5 h / 0 °C
3.1: sodium hydroxide / water / 0.75 h / 30 °C
3.2: 0.75 h / 35 °C
4.1: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
With
hydrogenchloride; water; oxalic acid; sodium hydroxide;
In
methanol; dichloromethane; water; acetonitrile;
|
|
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Multi-step reaction with 2 steps
1: hydrogenchloride / acetonitrile; water / 2 h / 13 °C
2: sodium hydroxide / water / 2 h / 10 °C / Large scale
With
hydrogenchloride; sodium hydroxide;
In
water; acetonitrile;
|
147511-69-1 Upstream products
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141750-58-5
(4R)-4,7,7-trimethyl-3-exo-(1-naphthyl)bicyclo<2.2.1>heptan-2-exo-yl (3S,5R,6E)-7-<2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl>-3,5-dihydroxy-6-heptenoate
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172336-32-2
(±)-E-3,5-dihydroxy-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-6-heptenoic acid ethyl ester
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121660-11-5
2-cyclopropyl-4-(4-fluorophenyl)-3-(hydroxymethyl)quinoline
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121660-37-5
2-cyclopropyl-4-(4-fluorophenyl)-3-formylquinoline
147511-69-1 Downstream products
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141750-59-6
(3S,5R,6E)-7-<2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl>-3,5-dihydroxy-6-heptenoic acid ,15-lactone
