TIANFU-CHEM - Irbesartan CAS NO.138402-11-6

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Product Details

Keywords

Irbesartan
138402-11-6
C25H28N6O

Quick Details

ProName: TIANFU-CHEM - Irbesartan
CasNo: 138402-11-6
Molecular Formula: C25H28N6O
Appearance: Solid
Application: Organic synthesis
DeliveryTime: PROMPT
PackAge: IN 25kg drums
Port: SHANGHAI
ProductionCapacity: 10 Metric Ton/Month
Purity: 99.0%
Storage: In Room Temperature
Transportation: As per MSDS
LimitNum: 1 Gram
Heavy metal: N/A
Grade: Industrial Grade,Food Grade,Pharma Gra...

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Henan Tianfu Chemical Co., Ltd. is located in Zhengzhou High-tech Development Zone with import and export license.

We passed ISO 9001:2008 in 2009, and won "High-tech Enterprise" by provincial government in 2013.The objective of the company is to put quality first and put our customer’s needs first - the satisfaction of our customers is the company's ultimate goal.

Improving product quality and service level is our responsibility, and creating more value for our customer’s is our purpose. We are constantly striving to make Henan Tianfu a leading chemical supplier, and hope to create a better future with you.

Details

Irbesartan Basic information

Antihypertensives Telmisartan Usage and Dosage Drug interaction Overdose Side effects Chemical property Uses Production Method

Product Name: Irbesartan

Synonyms: 3-butyl-2-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-2,4-diazaspiro[4.4]non-3-en-1-one;2-BUTYL-3-[[2'-(1H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL]METHYL]-1,3-DIAZASPIRO[4.4]NON-1-EN-4-ONE;IRBESARTAN;BMS-186295;AVAPRO;APROVEL;SR-47436;Lrbesartan

CAS: 138402-11-6

MF: C25H28N6O

MW: 428.53

EINECS:

Product Categories: Active Pharmaceutical Ingredients;Antihypertensive;Hypertension;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;API's;Aromatics;Heterocycles;Isotopically Labeled Pharmaceutical Reference Standard;LITAREX

Mol File: 138402-11-6.mol

Irbesartan Structure

Irbesartan Chemical Properties

Melting point 180-181°C

storage temp. -20°C Freezer

solubility DMSO: >25mg/mL

color white to off-white

Merck 14,5083

CAS DataBase Reference 138402-11-6(CAS DataBase Reference)

Safety Information

Hazard Codes Xn

Risk Statements 22

Safety Statements 26-24/25

RTECS HM2950270

MSDS Information

Provider Language

3-Butyl-2-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-2,4-diazaspiro[4.4]non-3-en-1-one English

Irbesartan Usage And Synthesis

Antihypertensives Irbesartan is an angiotensin Ⅱreceptor inhibitor, angiotensin Ⅱ receptors are divided into AT1, AT2, irbesartan can inhibit AngⅠtransform into AngⅡby selectively blocking the AT1 receptor of AngⅡ, specifically antagonize angiotensin converting enzyme 1 receptor (AT1), the antagonism of AT1 is 8500 times than that of AT2, it can inhibit vasoconstriction and aldosterone release by selectively blocking the binding AngⅡ with AT1 receptor and result in the antihypertensive effect. This product does not inhibit angiotensin converting enzyme (ACE), renin, and other hormone receptors, neither suppress the blood pressure regulation and the balance of sodium ion channels. Irbesartan can also reduce electrical remodeling of the myocardium, thereby reduce the mortality rate of patients with hypertension, it is the most effective drug for treatment of hypertension and cardiovascular disease.

Angiotensin antagonists (ARB) is applied to the clinical treatment of hypertension and diabetic nephropathy. At present, domestic drugs for treating high blood pressure are divided into angiotensin converting enzyme inhibitors (ACEI), calcium channel blockers, beta blockers and so on according to different working parts. By contrast, ARB has better antihypertensive effect, while Irbesartan is a new type of angiotensin antagonist which has clear antihypertensive effect, and has an important role in inhibiting left ventricular hypertrophy and protecting the kidneys.

According to foreign reports, it can quickly absorb by oral and the bioavailability is 60-80%, not affected by food. Plasma tmax is 1-1.5 hours, plasma protein combined rate is 90%, elimination half-life is 11-15 hours, reaching steady state in three days. By aldehyde oxidation acidification or glucose metabolism, vitro studies have shown that mainly oxidation by cytochrome enzymes of P450 and 2C9. This product and its metabolites excrete by biliary tract and kidney.

Irbesartan (Emberd) produced by Sanofi-aventis hangzhou minsheng pharmaceutical co., LTD won the approval of the SFDA used in the treatment of hypertension in type 2 diabetic nephropathy on March 8, 2007, and becomes China's first effective antihypertensive drug.

Telmisartan Telmisartan is a new type of blood pressure drug, is a kind of specific angiotensin Ⅱ receptor (AT Ⅰ) antagonist, used in the treatment of essential hypertension. To instead of high affinity of angiotensin receptor Ⅱwith AT Ⅰ receptor subtypes (known angiotensin Ⅱ loci). Telmisartan has no effects in the AT Ⅰ receptor agonist sites, selectively combined with ATⅠ receptor and the combined effect is durable. Has no affinity with other receptor (including AT2 and other characteristics of less AT receptors). The other receptor function remains to be seen, excessive receptor stimulation effect due to telmisartan angiotensin Ⅱ level is also not known. Telmisartan is not inhibit human plasma renin, and also don't block the ion channel. Don't inhibit angiotensin converting enzymeⅡ, the enzyme can degrade and enhance adverse reactions caused by the excitation peptide inhibition. 80 mg of telmisartan in the human body is almost completely inhibit angiotensin Ⅱ causing increased blood pressure. Inhibition effect is last for a full of 24 hours and can still be detectable in 48 hours. Antihypertensive effect is obvious in 3 hours after the first dose. At 4 weeks after treatment began to gain maximum antihypertensive effect, and can be maintained in the long-term treatment. If the treatment was interrupted suddenly, the blood pressure returns to the treatment level in just a few days, rather than a resilient high blood pressure. In direct comparison of two kinds of high blood pressure drugs in clinical trials, treatment group was significantly lower than that of patients with dry cough angiotensin converting enzyme inhibitors in treatment group.

The above information is edited by the Chemicalbook of Duan Yalan.

Usage and Dosage Oral: recommended starting dose of 0.15 g, 1 time a day. It can be increased to 0.3 g according to the condition, 1 time a day. Can be used alone, also can be shared with other anti-hypertensive drugs.

Severe hypertension and not satisfied with drop in blood pressure after the drug increment, can add with small dose of diuretic (such as thiazide) or other antihypertensive drugs.

Drug interaction It has no obvious interactions with hydrochlorothiazide, digoxin, warfarin, nitrate benzene, pyridine.

It should be paid attention to when shared with diuretics due to insufficient blood volume and low sodium which can cause low blood pressure (hypotension). When shared with potassium diuretics (such as ammonia, benzene with organism), should avoid potassium increasing.

Do not affect each other pharmacokinetics when shared with digitalis drugs such as digoxin, beta blockers such as atenolol, calcium antagonists such as benzene, pyridine nitrate.

Overdose After an overdose of this product can occur hypotension, tachycardia or bradycardia, vomiting, gastric lavage and support therapy should be adopted.

Side effects Common adverse reactions: headache, dizziness, palpitation, etc., I have a cough, general degree is slight, the majority of patients continue to drugs are tolerated.

Rare urticaria and angioneurotic oedema.

Literature on this product is: the incidence of adverse reactions to more than 1% of indigestion, stomach burning, diarrhea, skeletal muscle pain, fatigue, and upper respiratory tract infection, but with the blank control group no significant difference.

Greater than 1% but less than control group in the incidence of abdominal pain, anxiety, nervousness, nausea, vomiting, chest pain, pharyngitis, skin rashes, tachycardia, etc. Low blood pressure and incidence of orthostatic hypotension is about 0.4%.

Chemical property Crystallization from 96% ethanol, melting point is 180-181 ℃.

Uses Antihypertensive drugs. Angiotensin Ⅱ-l (Ⅱ 1 A) receptor antagonist. Used to treat high blood pressure.

Production Method Methods 1:

1-(fluorene methoxy carbonyl amino) ring e carboxylic acid (I) benzylamine reaction with 4-(2-phenyl cyano) amidation, product (Ⅲ) and water release N to produce compound (Ⅳ). (Ⅳ) and Triethyl orthobutyrate condensation, cyclization to compound (V), then azide to formation tetrazolium with sodium reaction to obtain Telmisartan.

Methods 2:

1-(fluorene methoxyl carbonyl amino) ring e carboxylic acid (I) condensation with compound(Ⅳ), the product remove N protection based to compound (Ⅷ), reacts with Triethyl orthobutyrate, obtain the product.

Chemical Properties Crystalline Solid

Uses An angiotensin II type 1 (AII1)-receptor antagonist

Uses antidepressant

Uses For the treatment of hypertension, as well as diabetic nephropathy with an elevated serum creatinine and proteinuria (>300 mg/day) in patients with type 2 diabetes and hypertension. Irbesartan is also used as a second line agent in the treatment of conges

Definition ChEBI: A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.

Irbesartan Preparation Products And Raw materials

Raw materials Sodium azide-->Benzylamine-->Fluorene-->3-METHOXYPROPIONIC ACID-->Tetrazole-->ORTHO-N-VALERIC ACID TRIETHYL ESTER-->Triethyl orthobutyrate

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