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147526-32-7 Usage

Uses

Pitavastatin calcium (Livalo) is a novel member of the medication class of statins

Chemical Properties

White to Off-White Powder

Uses

A competitive inhibitor of HMG-CoA reductase.

Statin lipid-lowering drugs

Pitavastatin calcium is jointly developed by two companies Nissan Chemical and Kowa Co.it is the first total synthesis HMG-CoA reductase inhibitor, it belongs to statin drugs ,it reduces the ability of the liver to manufacture cholesterol mainly through inhibition of some liver enzymes called HMGCo-A reductase , thus it improves the elevated blood cholesterol levels, it is primarily used for the treatment of hypercholesterolemia and familial hypercholesterolemia patients,its lipid-lowering effect is very good, it is the most potent lipid-lowering drug so far.

Pharmacokinetics

The main parts of its absorption after oral administration are the duodenum and colon,its rate of binding plasma protein in the body is 96%and it is more selectively distributed in the liver after absorption , the drug concentration in body tissues is lower than that in the plasma or the same as that in the plasma . Pitavastatin calcium is mainly metabolized in the liver, kidney, lung, heart, muscle , metabolite concentrations are lower than the concentration of drug prototype, it is excreted through feces,there is also a small amount of drug excretion through urine , total excretion rate is almost 100%.
A healthy male adult oral pitavastatin is 0.5~8mg, t1/2 is about 10h,the cmax and AUC of the prototype drug in plasma increase with increasing dose , repeatedly taking does not result in medication savings.

Definition

ChEBI: The calcium salt of pitavastatin. Used for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise.

Clinical Study

In the therapeutic effect, statins is the first In the lipid-lowering drugs in which pitavastatin effect is very obvious, pitavastatin calcium is a third generation statins anti-hyperlipidemia drug, and Russell atorvastatin (rosuvastatin ) while being called "super statin", is one of the better statins which are current international clinical application of the treatment of hypercholesterolemia, familial hypercholesterolemia , because its clinically effective dose is 1-2mg/day, significantly lower than other marketed statins, with high efficiency, and security features, it has a good tolerability. clinical trail phase I results show that pitavastatin calcium in 1,2,4 mg dose has clinical significance in patients with high blood cholesterol.
Results of clinical trail phase Ⅱ determine that the best dosage of the pitavastatin calcium for the treatment of hyperlipidemia is 2mg/d.
clinical trail phaseⅢ comparison of experimental results show that the efficacy of pitavastatin calcium on reducing Tc and LDL-c is better than the effect of fluvastatin, and there is no significant difference in safety. Multi-center long-term administration tests carried out in Japan show that the dosage in 1~4mg/d range can effectively control blood lipid levels. The above test results demonstrate the effectiveness of pitavastatin calcium in treatment of hyperlipidemia on clinic.

Pharmacological effects

Inhibition of HMG-CoA reductase: pitavastatin calcium has a strongly antagonistic inhibition effect on HMG-CoA enzyme , IC50 value is 6.8 nmol/L, and its intensity is 24 times of simvastatin, while it is 68 times of fluvastatin.
It Hinders the synthesis of cholesterol: the ability to effectively inhibit the process of generating cholesterol in human hepatocytes HepG2 , IC50 value is 5.8nmol/L, and its intensity is 29 times of simvastatin, it is 57 times that of atorvastatin. But pitavastatin calcium inhibition effect on each enzyme in cholesterol generation after generation of mevalonate is very weak.
It Increases LDL receptor density: pitavastatin induces the synthesis of LDS receptor mRNA in the ultra-low concentration of 1μmol/L, it can increase the number of LDS receptor mRNA , it results in the increasing of LDL receptor density , thereby it promotes clearance of LDL , so that plasma LDL-plasma total cholesterol concentration and triglyceride concentration decrease.
The above information is edited by the Chemicalbook of Tian Ye.

Toxicity

Acute toxicity: rats and dogs oral,study its acute toxicity. Pitavastatin calcium median lethal dose on the rats are about male 500~1000mg/kg, female 250~500 mg/kg, dogs lethal dose is about 50~100mg/kg.
Long term toxicity: respectively, rats, dogs and monkeys are administered a long-term experiment. From the experimental results, the safe dose of pitavastatin calcium are rats 1 mg/kg · d-1 (6 months), canine 0.3mg/kg · d-1 (12 months), monkey 3mg/kg · d-1 (6 months). No central nervous system, reproductive system, and myocardial dysfunction is observed which is common while taking other statins during administration.
Carcinogenicity, mutagenicity: mouse oral 1,12,30, 75mg/kg dose, the incidence of cancer has no significant increase than in the control group .in Chromosome abnormality tests, at the highest concentration of 625μg/ml,the result is positive, but at the same concentration, gene mutation recovery tests, micronucleus test s(in vivo) and UDS test s(in vivo) are negative.
InChI:InChI=1/2C25H25FNO4.Ca/c2*26-17-9-7-15(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;/h2*1-4,7-12,16,18-19,23,28-30H,5-6,13-14H2;/q2*-1;+2/b2*12-11+;/t2*18-,19-,23+;/m11./s1

147526-32-7SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 19, 2017

Revision Date: Aug 19, 2017

1.Identification

1.1 GHS Product identifier

Product name pitavastatin calcium

1.2 Other means of identification

Product number -
Other names UNII-IYD54XEG3W

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:147526-32-7 SDS

147526-32-7Synthetic route

methyl (3R,5S,6E)-7-{2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl}-3,5-dihydroxyhept-6-enoate
849811-78-5

methyl (3R,5S,6E)-7-{2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl}-3,5-dihydroxyhept-6-enoate

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
With sodium hydroxide In methanol at 20℃; for 0.5h;100%
With water; sodium hydroxide In methanol at 20℃; for 2h; Product distribution / selectivity;
pitavastatin calcium salt
147526-32-7

pitavastatin calcium salt

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
With hydrogenchloride In water; ethyl acetate at 25 - 35℃;95.9%
With hydrogenchloride In dichloromethane; water at 0 - 25℃; for 0.833333h; pH=3;
With hydrogenchloride In water; ethyl acetate pH=4;3.7 g
With hydrogenchloride In dichloromethane; water
(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
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

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Stage #1: (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℃;
Stage #2: With caesium carbonate In acetonitrile at 35 - 40℃;
94%
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
View Scheme
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
View Scheme
Multi-step reaction with 2 steps
1: hydrogenchloride / acetonitrile; water / 2 h / 13 °C
2: sodium hydroxide / water / 2 h / 10 °C / Large scale
View Scheme
(E)-(3R,5S)-7-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-3,5-dihydroxy-hept-6-enoic acid ethyl ester
167073-19-0

(E)-(3R,5S)-7-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-3,5-dihydroxy-hept-6-enoic acid ethyl ester

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
With ethanol; sodium hydroxide In water at 20℃; for 3h;87.4%
(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-3,5-dihydroxy-6-heptenoic 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

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
With sodium hydroxide In water at 10℃; for 2h; Large scale;83.9%
Stage #1: (3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-3,5-dihydroxy-6-heptenoic acid tert-butyl ester With hydrogenchloride; water In methanol at 25℃; for 2.16667h;
Stage #2: With hydrogenchloride In dichloromethane at 0 - 25℃; for 0.916667h; pH=3;
Multi-step reaction with 2 steps
1.1: sodium hydroxide; water / methanol / 1.67 h / 0 °C
1.2: 0.67 h / 25 °C
2.1: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
View Scheme
Multi-step reaction with 3 steps
1.1: sodium hydroxide; water / acetonitrile / 1.5 h / 30 °C
1.2: 0.25 h / 0 °C / pH 4
1.3: 0.5 h / 0 °C
2.1: sodium hydroxide / water / 0.75 h / 30 °C
2.2: 0.75 h / 35 °C
3.1: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
View Scheme
(4R)-4,7,7-trimethyl-3-exo-(1-naphthyl)bicyclo<2.2.1>heptan-2-exo-yl (3R,5S,6E)-7-<2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl>-3,5-dihydroxy-6-heptenoate

(4R)-4,7,7-trimethyl-3-exo-(1-naphthyl)bicyclo<2.2.1>heptan-2-exo-yl (3R,5S,6E)-7-<2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl>-3,5-dihydroxy-6-heptenoate

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
With sodium hydroxide In methanol for 12h; Ambient temperature;
(±)-E-3,5-dihydroxy-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-6-heptenoic acid ethyl ester

(±)-E-3,5-dihydroxy-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-6-heptenoic acid ethyl ester

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Stage #1: (±)-E-3,5-dihydroxy-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-6-heptenoic acid ethyl ester With sodium hydroxide Hydrolysis;
Stage #2: With (+)-1-phenylethylamine resolution;
(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxy-[(1S)-1-phenylethyl]hept-6-enamide

(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxy-[(1S)-1-phenylethyl]hept-6-enamide

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Stage #1: (3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxy-[(1S)-1-phenylethyl]hept-6-enamide With sodium hydroxide In ethanol at 50 - 55℃; for 26h;
Stage #2: With hydrogenchloride In ethyl acetate Further stages.;
2-cyclopropyl-4-(4-fluorophenyl)-3-(hydroxymethyl)quinoline
121660-11-5

2-cyclopropyl-4-(4-fluorophenyl)-3-(hydroxymethyl)quinoline

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: DMSO; P2O5; Et3N
2.1: NaOH; (n-octyl)3MeNCl / toluene; H2O
3.1: DIBAH
4.1: NaH; n-BuLi
5.1: NaBH4; Et2BOMe / -78 °C
6.1: aq. NaOH
6.2: (+)-α-methylbenzylamine
View Scheme
Multi-step reaction with 4 steps
1.1: phosphorus tribromide / dichloromethane / 1.5 h / 25 °C
1.2: 1 h / 75 °C
2.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
3.1: water; oxalic acid / methanol / 6 h / 35 °C
3.2: 2.75 h / 10 - 30 °C / pH 7
4.1: hydrogenchloride; water / methanol / 2.17 h / 25 °C
4.2: 0.92 h / 0 - 25 °C / pH 3
View Scheme
Multi-step reaction with 5 steps
1.1: phosphorus tribromide / dichloromethane / 1.5 h / 25 °C
1.2: 1 h / 75 °C
2.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
3.1: water; oxalic acid / methanol / 6 h / 35 °C
3.2: 2.75 h / 10 - 30 °C / pH 7
4.1: sodium hydroxide; water / methanol / 1.67 h / 0 °C
4.2: 0.67 h / 25 °C
5.1: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
View Scheme
Multi-step reaction with 6 steps
1.1: phosphorus tribromide / dichloromethane / 1.5 h / 25 °C
1.2: 1 h / 75 °C
2.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
3.1: water; oxalic acid / methanol / 6 h / 35 °C
3.2: 2.75 h / 10 - 30 °C / pH 7
4.1: sodium hydroxide; water / acetonitrile / 1.5 h / 30 °C
4.2: 0.25 h / 0 °C / pH 4
4.3: 0.5 h / 0 °C
5.1: sodium hydroxide / water / 0.75 h / 30 °C
5.2: 0.75 h / 35 °C
6.1: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
View Scheme
Multi-step reaction with 5 steps
1: thionyl chloride / toluene; dichloromethane / 15 °C
2: toluene / 12 h / Reflux; Large scale
3: potassium carbonate / dimethyl sulfoxide / 3 h / 30 - 50 °C / Large scale
4: hydrogenchloride / acetonitrile; water / 2 h / 13 °C
5: sodium hydroxide / water / 2 h / 10 °C / Large scale
View Scheme
2-cyclopropyl-4-(4-fluorophenyl)-3-formylquinoline
121660-37-5

2-cyclopropyl-4-(4-fluorophenyl)-3-formylquinoline

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: NaOH; (n-octyl)3MeNCl / toluene; H2O
2.1: DIBAH
3.1: NaH; n-BuLi
4.1: NaBH4; Et2BOMe / -78 °C
5.1: aq. NaOH
5.2: (+)-α-methylbenzylamine
View Scheme
Multi-step reaction with 3 steps
1.1: sodium t-butanolate / 1-methyl-pyrrolidin-2-one; 2-methyltetrahydrofuran; tetrahydrofuran / -60 - 22 °C
2.1: hydrogenchloride / acetonitrile; water / 1.5 h / 45 °C
2.2: 1.5 h
3.1: hydrogenchloride / water; ethyl acetate / pH 4
View Scheme
Multi-step reaction with 4 steps
1.1: sodium t-butanolate / 1-methyl-pyrrolidin-2-one; 2-methyltetrahydrofuran; tetrahydrofuran / -60 - 22 °C
2.1: hydrogenchloride / acetonitrile; water / 2.5 h / 45 °C
2.2: 1.5 h / 10 °C
3.1: sodium hydroxide / water / pH 12.3
3.2: 1.25 h / pH 9.7
4.1: hydrogenchloride / water; ethyl acetate / pH 4
View Scheme
(E)-3-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-propenal
148901-68-2

(E)-3-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-propenal

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: NaH; n-BuLi
2.1: NaBH4; Et2BOMe / -78 °C
3.1: aq. NaOH
3.2: (+)-α-methylbenzylamine
View Scheme
(E)-3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]-2-propenenitrile
256431-72-8

(E)-3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]-2-propenenitrile

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: DIBAH
2.1: NaH; n-BuLi
3.1: NaBH4; Et2BOMe / -78 °C
4.1: aq. NaOH
4.2: (+)-α-methylbenzylamine
View Scheme
(E)-7-[2-cyclopropyl-4-(4-fluorophenyl)-quinolin-3-yl]-5-hydroxy-3-oxohept-6-enic 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

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: NaBH4; Et2BOMe / -78 °C
2.1: aq. NaOH
2.2: (+)-α-methylbenzylamine
View Scheme
With Candida rugosa IFO0591 In dimethyl sulfoxide at 30℃; for 20h; pH=7; Product distribution / selectivity; Aerobic conditions; potassium phosphate buffer (pH 7.0);n/a
With Candida molischiana IFO10296 In dimethyl sulfoxide at 30℃; for 20h; pH=7; Product distribution / selectivity; Aerobic conditions; potassium phosphate buffer (pH 7.0);n/a
(E)-7-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-3,5-dioxo-hept-6-enoic acid ethyl ester
166803-31-2

(E)-7-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-3,5-dioxo-hept-6-enoic acid ethyl ester

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
With Candida famata RIFY7455 In dimethyl sulfoxide at 30℃; for 20h; pH=7; Product distribution / selectivity; Aerobic conditions; potassium phosphate buffer (pH 7.0);n/a
With Candida albicans IFO1594 In dimethyl sulfoxide at 30℃; for 20h; pH=7; Product distribution / selectivity; Aerobic conditions; potassium phosphate buffer (pH 7.0);n/a
With Candida parapsilosis CBS604 In dimethyl sulfoxide at 30℃; for 20h; pH=7; Product distribution / selectivity; Aerobic conditions; potassium phosphate buffer (pH 7.0);n/a
(R)-1-benzyl 7-methyl 5-(tert-butyldimethylsilyloxy)-3-oxoheptanedioate
1343494-43-8

(R)-1-benzyl 7-methyl 5-(tert-butyldimethylsilyloxy)-3-oxoheptanedioate

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: hydrogen / palladium 10% on activated carbon / ethyl acetate / 2 h / 20 °C / Inert atmosphere
2.1: piperidine / N,N-dimethyl-formamide / 10.25 h / 20 - 40 °C / Inert atmosphere
3.1: hydrogenchloride / water; methanol / 0 - 20 °C
4.1: sodium tetrahydroborate; diethyl methoxy borane / tetrahydrofuran; methanol / 0.5 h / -78 °C
4.2: 1 h / 50 °C
5.1: sodium hydroxide; water / methanol / 2 h / 20 °C
View Scheme
(R)-5-(tert-butyldimethylsilyloxy)-7-methoxy-3,7-dioxoheptanoic acid
1343494-44-9

(R)-5-(tert-butyldimethylsilyloxy)-7-methoxy-3,7-dioxoheptanoic acid

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: piperidine / N,N-dimethyl-formamide / 10.25 h / 20 - 40 °C / Inert atmosphere
2.1: hydrogenchloride / water; methanol / 0 - 20 °C
3.1: sodium tetrahydroborate; diethyl methoxy borane / tetrahydrofuran; methanol / 0.5 h / -78 °C
3.2: 1 h / 50 °C
4.1: sodium hydroxide; water / methanol / 2 h / 20 °C
View Scheme
(R,E)-methyl 3-(tert-butyldimethylsilyloxy)-7-(2-cyclopropyl-4-(-4-fluorophenyl)-quinolin-3-yl)-5-oxohept-6-enoate

(R,E)-methyl 3-(tert-butyldimethylsilyloxy)-7-(2-cyclopropyl-4-(-4-fluorophenyl)-quinolin-3-yl)-5-oxohept-6-enoate

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: hydrogenchloride / water; methanol / 0 - 20 °C
2.1: sodium tetrahydroborate; diethyl methoxy borane / tetrahydrofuran; methanol / 0.5 h / -78 °C
2.2: 1 h / 50 °C
3.1: sodium hydroxide; water / methanol / 2 h / 20 °C
View Scheme
Cyclopropyl methyl ketone
765-43-5

Cyclopropyl methyl ketone

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: toluene / 0.25 h / 25 °C
1.2: 14 h / 10 - 75 °C / Inert atmosphere
1.3: 0.75 h / 0 - 25 °C / pH 2.5
2.1: sulfuric acid / water; methanol / 22.25 h / 25 - 65 °C
2.2: 0.75 h / 0 - 25 °C / pH 6
3.1: toluene / 5 h / 25 °C / Inert atmosphere
3.2: 3 h
3.3: 2 h / 40 °C
4.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
5.1: water; oxalic acid / methanol / 6 h / 35 °C
5.2: 2.75 h / 10 - 30 °C / pH 7
6.1: hydrogenchloride; water / methanol / 2.17 h / 25 °C
6.2: 0.92 h / 0 - 25 °C / pH 3
View Scheme
Multi-step reaction with 7 steps
1.1: toluene / 0.25 h / 25 °C
1.2: 14 h / 10 - 75 °C / Inert atmosphere
1.3: 0.75 h / 0 - 25 °C / pH 2.5
2.1: sulfuric acid / water; methanol / 22.25 h / 25 - 65 °C
2.2: 0.75 h / 0 - 25 °C / pH 6
3.1: toluene / 5 h / 25 °C / Inert atmosphere
3.2: 3 h
3.3: 2 h / 40 °C
4.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
5.1: water; oxalic acid / methanol / 6 h / 35 °C
5.2: 2.75 h / 10 - 30 °C / pH 7
6.1: sodium hydroxide; water / methanol / 1.67 h / 0 °C
6.2: 0.67 h / 25 °C
7.1: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
View Scheme
Multi-step reaction with 7 steps
1.1: toluene / 0.25 h / 25 °C
1.2: 14 h / 10 - 75 °C / Inert atmosphere
1.3: 0.75 h / 0 - 25 °C / pH 2.5
2.1: sulfuric acid / water; methanol / 22.25 h / 25 - 65 °C
2.2: 0.75 h / 0 - 25 °C / pH 6
3.1: diisobutylaluminium hydride / toluene / 2 h / 0 - 25 °C
3.2: 0.25 h / 10 °C
4.1: phosphorus tribromide / dichloromethane / 1.5 h / 25 °C
4.2: 1 h / 75 °C
5.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
6.1: water; oxalic acid / methanol / 6 h / 35 °C
6.2: 2.75 h / 10 - 30 °C / pH 7
7.1: hydrogenchloride; water / methanol / 2.17 h / 25 °C
7.2: 0.92 h / 0 - 25 °C / pH 3
View Scheme
methyl 3-cyclopropyl-3-oxopropanoate
32249-35-7

methyl 3-cyclopropyl-3-oxopropanoate

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: sulfuric acid / water; methanol / 22.25 h / 25 - 65 °C
1.2: 0.75 h / 0 - 25 °C / pH 6
2.1: toluene / 5 h / 25 °C / Inert atmosphere
2.2: 3 h
2.3: 2 h / 40 °C
3.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
4.1: water; oxalic acid / methanol / 6 h / 35 °C
4.2: 2.75 h / 10 - 30 °C / pH 7
5.1: hydrogenchloride; water / methanol / 2.17 h / 25 °C
5.2: 0.92 h / 0 - 25 °C / pH 3
View Scheme
Multi-step reaction with 6 steps
1.1: sulfuric acid / water; methanol / 22.25 h / 25 - 65 °C
1.2: 0.75 h / 0 - 25 °C / pH 6
2.1: toluene / 5 h / 25 °C / Inert atmosphere
2.2: 3 h
2.3: 2 h / 40 °C
3.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
4.1: water; oxalic acid / methanol / 6 h / 35 °C
4.2: 2.75 h / 10 - 30 °C / pH 7
5.1: sodium hydroxide; water / methanol / 1.67 h / 0 °C
5.2: 0.67 h / 25 °C
6.1: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
View Scheme
Multi-step reaction with 6 steps
1.1: sulfuric acid / water; methanol / 22.25 h / 25 - 65 °C
1.2: 0.75 h / 0 - 25 °C / pH 6
2.1: diisobutylaluminium hydride / toluene / 2 h / 0 - 25 °C
2.2: 0.25 h / 10 °C
3.1: phosphorus tribromide / dichloromethane / 1.5 h / 25 °C
3.2: 1 h / 75 °C
4.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
5.1: water; oxalic acid / methanol / 6 h / 35 °C
5.2: 2.75 h / 10 - 30 °C / pH 7
6.1: hydrogenchloride; water / methanol / 2.17 h / 25 °C
6.2: 0.92 h / 0 - 25 °C / pH 3
View Scheme
methyl 4-(4'-fluorophenyl)-2-cyclopropylquinoline-3-carboxylate
121659-86-7

methyl 4-(4'-fluorophenyl)-2-cyclopropylquinoline-3-carboxylate

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: toluene / 5 h / 25 °C / Inert atmosphere
1.2: 3 h
1.3: 2 h / 40 °C
2.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
3.1: water; oxalic acid / methanol / 6 h / 35 °C
3.2: 2.75 h / 10 - 30 °C / pH 7
4.1: hydrogenchloride; water / methanol / 2.17 h / 25 °C
4.2: 0.92 h / 0 - 25 °C / pH 3
View Scheme
Multi-step reaction with 5 steps
1.1: toluene / 5 h / 25 °C / Inert atmosphere
1.2: 3 h
1.3: 2 h / 40 °C
2.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
3.1: water; oxalic acid / methanol / 6 h / 35 °C
3.2: 2.75 h / 10 - 30 °C / pH 7
4.1: sodium hydroxide; water / methanol / 1.67 h / 0 °C
4.2: 0.67 h / 25 °C
5.1: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
View Scheme
Multi-step reaction with 5 steps
1.1: diisobutylaluminium hydride / toluene / 2 h / 0 - 25 °C
1.2: 0.25 h / 10 °C
2.1: phosphorus tribromide / dichloromethane / 1.5 h / 25 °C
2.2: 1 h / 75 °C
3.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
4.1: water; oxalic acid / methanol / 6 h / 35 °C
4.2: 2.75 h / 10 - 30 °C / pH 7
5.1: hydrogenchloride; water / methanol / 2.17 h / 25 °C
5.2: 0.92 h / 0 - 25 °C / pH 3
View Scheme
pitavastatin methyl amine salt

pitavastatin methyl amine salt

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: sodium hydroxide / water / 0.75 h / 30 °C
1.2: 0.75 h / 35 °C
2.1: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
View Scheme
<2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl>methyltriphenylphosphonium bromide

<2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl>methyltriphenylphosphonium bromide

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
2.1: water; oxalic acid / methanol / 6 h / 35 °C
2.2: 2.75 h / 10 - 30 °C / pH 7
3.1: hydrogenchloride; water / methanol / 2.17 h / 25 °C
3.2: 0.92 h / 0 - 25 °C / pH 3
View Scheme
Multi-step reaction with 4 steps
1.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
2.1: water; oxalic acid / methanol / 6 h / 35 °C
2.2: 2.75 h / 10 - 30 °C / pH 7
3.1: sodium hydroxide; water / methanol / 1.67 h / 0 °C
3.2: 0.67 h / 25 °C
4.1: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
View Scheme
Multi-step reaction with 5 steps
1.1: potassium carbonate / dimethyl sulfoxide / 7 h / 75 °C
2.1: water; oxalic acid / methanol / 6 h / 35 °C
2.2: 2.75 h / 10 - 30 °C / pH 7
3.1: sodium hydroxide; water / acetonitrile / 1.5 h / 30 °C
3.2: 0.25 h / 0 °C / pH 4
3.3: 0.5 h / 0 °C
4.1: sodium hydroxide / water / 0.75 h / 30 °C
4.2: 0.75 h / 35 °C
5.1: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
View Scheme
(E)-3(R)-5(S)-dihydroxy-7-[4'-(4-fluorophenyl)-2'-cyclopropylquinoline-3'-yl]hept-6-eneacidD(+)phenylethylamine salt
1392469-74-7

(E)-3(R)-5(S)-dihydroxy-7-[4'-(4-fluorophenyl)-2'-cyclopropylquinoline-3'-yl]hept-6-eneacidD(+)phenylethylamine salt

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: sodium hydroxide; calcium chloride / water
2: hydrogenchloride / dichloromethane; water / 0.83 h / 0 - 25 °C / pH 3
View Scheme
2-((4R,6S)-6-((E)-2-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)vinyl)-2,2-dimethyl-1 ,3-dioxan-4-yl)acetate methyl ester

2-((4R,6S)-6-((E)-2-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)vinyl)-2,2-dimethyl-1 ,3-dioxan-4-yl)acetate methyl ester

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: hydrogenchloride / acetonitrile; water / 1.5 h / 45 °C
1.2: 1.5 h
2.1: hydrogenchloride / water; ethyl acetate / pH 4
View Scheme
Multi-step reaction with 3 steps
1.1: hydrogenchloride / acetonitrile; water / 2.5 h / 45 °C
1.2: 1.5 h / 10 °C
2.1: sodium hydroxide / water / pH 12.3
2.2: 1.25 h / pH 9.7
3.1: hydrogenchloride / water; ethyl acetate / pH 4
View Scheme
2-((4R,6S)-6-((benzo[d]thiazol-2-ylsulfonyl)methyl)-2,2-dimethyl-1,3-dioxan-4-yl)acetic acid methyl ester
1388627-65-3

2-((4R,6S)-6-((benzo[d]thiazol-2-ylsulfonyl)methyl)-2,2-dimethyl-1,3-dioxan-4-yl)acetic acid methyl ester

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: sodium t-butanolate / 1-methyl-pyrrolidin-2-one; 2-methyltetrahydrofuran; tetrahydrofuran / -60 - 22 °C
2.1: hydrogenchloride / acetonitrile; water / 1.5 h / 45 °C
2.2: 1.5 h
3.1: hydrogenchloride / water; ethyl acetate / pH 4
View Scheme
Multi-step reaction with 4 steps
1.1: sodium t-butanolate / 1-methyl-pyrrolidin-2-one; 2-methyltetrahydrofuran; tetrahydrofuran / -60 - 22 °C
2.1: hydrogenchloride / acetonitrile; water / 2.5 h / 45 °C
2.2: 1.5 h / 10 °C
3.1: sodium hydroxide / water / pH 12.3
3.2: 1.25 h / pH 9.7
4.1: hydrogenchloride / water; ethyl acetate / pH 4
View Scheme
pitavastatin-furfuryl amine salt

pitavastatin-furfuryl amine salt

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: sodium hydroxide / water / pH 12.3
1.2: 1.25 h / pH 9.7
2.1: hydrogenchloride / water; ethyl acetate / pH 4
View Scheme
C13H12BrNO

C13H12BrNO

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 7 steps
1.1: Dess-Martin periodane / dichloromethane / 3 h / 0 - 20 °C / Inert atmosphere
2.1: sodium hydride / tetrahydrofuran; mineral oil / 1 h / 0 °C / Inert atmosphere
2.2: 0 - 20 °C / Inert atmosphere
3.1: hydrogenchloride / acetonitrile / 19 h / 0 - 20 °C
4.1: diethyl methoxy borane; sodium tetrahydroborate / methanol; tetrahydrofuran / 1.33 h / -78 °C
4.2: 3 h / 20 °C
5.1: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2; potassium carbonate / dimethyl sulfoxide / 4 h / 70 °C / Inert atmosphere
6.1: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2; tetrakis(triphenylphosphine) palladium(0); sodium carbonate / dimethyl sulfoxide / 9 h / 90 °C / Inert atmosphere
7.1: sodium hydroxide / methanol / 0.5 h / 20 °C
View Scheme
anthranilic acid nitrile
1885-29-6

anthranilic acid nitrile

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 10 steps
1.1: tin(IV) chloride / toluene / 3 h / 15 °C / Inert atmosphere; Reflux
2.1: copper(I) bromide; tert.-butylnitrite / acetonitrile / 2.5 h / 15 - 40 °C / Inert atmosphere
3.1: diisobutylaluminium hydride / toluene; hexane / 1 h / 0 - 20 °C / Inert atmosphere
4.1: Dess-Martin periodane / dichloromethane / 3 h / 0 - 20 °C / Inert atmosphere
5.1: sodium hydride / tetrahydrofuran; mineral oil / 1 h / 0 °C / Inert atmosphere
5.2: 0 - 20 °C / Inert atmosphere
6.1: hydrogenchloride / acetonitrile / 19 h / 0 - 20 °C
7.1: diethyl methoxy borane; sodium tetrahydroborate / methanol; tetrahydrofuran / 1.33 h / -78 °C
7.2: 3 h / 20 °C
8.1: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2; potassium carbonate / dimethyl sulfoxide / 4 h / 70 °C / Inert atmosphere
9.1: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2; tetrakis(triphenylphosphine) palladium(0); sodium carbonate / dimethyl sulfoxide / 9 h / 90 °C / Inert atmosphere
10.1: sodium hydroxide / methanol / 0.5 h / 20 °C
View Scheme
methyl (4-amino-2-cyclopropylquinolin-3-yl)carboxylate

methyl (4-amino-2-cyclopropylquinolin-3-yl)carboxylate

pitavastatin
147526-32-7

pitavastatin

Conditions
ConditionsYield
Multi-step reaction with 9 steps
1.1: copper(I) bromide; tert.-butylnitrite / acetonitrile / 2.5 h / 15 - 40 °C / Inert atmosphere
2.1: diisobutylaluminium hydride / toluene; hexane / 1 h / 0 - 20 °C / Inert atmosphere
3.1: Dess-Martin periodane / dichloromethane / 3 h / 0 - 20 °C / Inert atmosphere
4.1: sodium hydride / tetrahydrofuran; mineral oil / 1 h / 0 °C / Inert atmosphere
4.2: 0 - 20 °C / Inert atmosphere
5.1: hydrogenchloride / acetonitrile / 19 h / 0 - 20 °C
6.1: diethyl methoxy borane; sodium tetrahydroborate / methanol; tetrahydrofuran / 1.33 h / -78 °C
6.2: 3 h / 20 °C
7.1: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2; potassium carbonate / dimethyl sulfoxide / 4 h / 70 °C / Inert atmosphere
8.1: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2; tetrakis(triphenylphosphine) palladium(0); sodium carbonate / dimethyl sulfoxide / 9 h / 90 °C / Inert atmosphere
9.1: sodium hydroxide / methanol / 0.5 h / 20 °C
View Scheme
pitavastatin
147526-32-7

pitavastatin

C25H22FNO3

C25H22FNO3

Conditions
ConditionsYield
With potassium tert-butylate In tetrahydrofuran at 5 - 20℃; Inert atmosphere;82%
pitavastatin
147526-32-7

pitavastatin

(3R,5S,6E)-7-<2-cyclopropyl-4-(4-fluorophenyl)-quinolin-3-yl>-3,5-dihydroxy-6-heptenoic acid 1,5-lactone

(3R,5S,6E)-7-<2-cyclopropyl-4-(4-fluorophenyl)-quinolin-3-yl>-3,5-dihydroxy-6-heptenoic acid 1,5-lactone

Conditions
ConditionsYield
With trifluoroacetic acid In dichloromethane at 0 - 30℃; for 3h;81%
In toluene for 1h; Heating;
berberine chloride
633-65-8

berberine chloride

pitavastatin
147526-32-7

pitavastatin

C25H23FNO4(1-)*C20H18NO4(1+)

C25H23FNO4(1-)*C20H18NO4(1+)

Conditions
ConditionsYield
With sodium hydroxide In ethanol; water at 60 - 70℃; pH=7 - 8;81%
pitavastatin
147526-32-7

pitavastatin

(±)-E-6-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-ylvinyl]-4-hydroxy-3,4,5,6-tetrahydrovalerolactone

(±)-E-6-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-ylvinyl]-4-hydroxy-3,4,5,6-tetrahydrovalerolactone

Conditions
ConditionsYield
In toluene for 12h; Heating; Yield given;
(R)-1-(1-Naphthyl)ethylamine
3886-70-2

(R)-1-(1-Naphthyl)ethylamine

pitavastatin
147526-32-7

pitavastatin

(3R,5S,E)-7-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoic acid (R)-NEA salt
1213706-08-1

(3R,5S,E)-7-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoic acid (R)-NEA salt

Conditions
ConditionsYield
In hexane; acetone at 20℃; for 16h;

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