Valsartan CAS 137862-53-4
Factory Supply Valsartan CAS 137862-53-4 with Best Price
- Appearance: White powder
- Purity: 99. 0%min
- Stock: In stock
- Sample: Available
- Zhishang Chemical: Valsartan Supplier & Manufacturer
Valsartan: The Complete Guide
Valsartan for Sale
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What is Valsartan?
Valsartan is a particular angiotensin II (AT1) receptor villain. It is additionally one more non-peptide AT1 receptor antagonist used medically after losartan. Equilibrium plays a vital role. It precisely acts upon the AT1 receptor subtype, blocking the binding of Ang II to the AT1 receptor (its particular antagonism on the AT1 receptor is about 20,000 times more than that of the AT2 receptor), thus hindering vasoconstriction as well as the release of aldosterone, generating Antihypertensive effect, but does not inhibit the launch of aldosterone brought on by potassium ions (K+). The antihypertensive effect is better than that of enalapril, and it appropriates for the treatment of antihypertensive, moderate to moderate vital hypertension, especially for secondary high blood pressure brought on by kidney damage, and can dramatically reduce hypertensive people with diabetic issues or typical renal feature Proteinuria in people with high blood pressure, and also has a renal protective impact of advertising uric acid and also urinary system salt discharging. Additionally suggested to minimize cardiovascular mortality in high threat clients (left ventricular failure or left ventricular disorder) after a cardiovascular disease.
A scientific test showed that valsartan was really effective in light to modest high blood pressure. A single day-to-day dose of ≥ 80 mg can efficiently manage systolic and also diastolic high blood pressure for 24-hour without transforming the rhythm of high blood pressure modifications; 160 mg once daily is extra effective than losartan 100 mg daily. Patients with moderate high blood pressure and also undamaged renal feature have great resistance to valsartan, the medicinal impact is significantly much better than that of converting enzyme inhibitors, and the adverse reactions are light. Combination with various other antihypertensive medicines is effective for extreme high blood pressure.
Valsartan Angiotensin Ⅱ belongs to one of the most critical active mediators of the renin-angiotensin-aldosterone system (RAAs) clinically. It can produce significant promoting effects on growth and structural variation. It has been confirmed that angiotensin Ⅱ can play a significant and important pathophysiological role in the occurrence of hypertension and target organ damage. Valsartan will selectively bind to the AT1 subtype, thereby blocking and inhibiting all the effects of Ang II that contribute to hypertension and related complications, including the generation of Ang II by non-ACE enzymatic reactions. In terms of hormone receptors, enzymes and ion channels produced by AngⅡ in system regulation, valsartan will not bind to them, nor will it produce blocking effects.
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Application of Valsartan
ARB drugs such as valsartan have only entered clinical practice for more than 10 years. As a new drug, evidence-based medical evidence and continuous in-depth basic research are needed to promote the clinical practice of ARB. As the first-line antihypertensive drug identified by WHO, valsartan has positive curative effect and few adverse reactions. Compared with other antihypertensive drugs, valsartan has unique advantages, and has broad application prospects in the prevention and treatment of hypertension, heart failure, myocardial infarction, diabetes, kidney disease, stroke, etc. clinical use.
Valsartan is an orally effective specific angiotensin II (AngII) type 1 receptor (ATl) antagonist, initially it was mainly used to treat hypertension, especially for secondary hypertension caused by renal damage . But with the progress of research and the renin. With the in-depth understanding of the angiotensin system (RAS), more and more evidence supports its application in diabetes, coronary heart disease, heart failure, acute myocardial infarction, etc. The publication of the results of Nateglinide and Valsartan on the Outcomes of Patients with Impaired Glucose Tolerance (NAVIGATOR) enriched the application of valsartan in the impaired glucose tolerance (IGT) population with cardiovascular disease or cardiovascular risk factors. Based on evidence-based medicine, it is believed that valsartan can improve glucose metabolism disorders and open up a new way for the prevention of type 2 diabetes (T2DM).
Preparation of Valsartan
- Preparation of cyclization reaction solution of valsartan methyl ester
Add 150ml of toluene and 40.65g (0.1mol) of N-(1-pentanoyl)-N-[4-[2-(5-cyano)phenyl]benzyl]-L-valamine in a 500ml four-necked flask Acid methyl ester (1), stirring, heating up (about 30°C) to compound (1-pentanoyl)-N-[4-[2-(5-cyano)phenyl]benzyl]-L-valline The acid methyl ester is completely dissolved. After the dissolution is complete, add 6.5g (0.1mol) sodium azide, 13.75g (0.1mol) triethylamine hydrochloride and 4g (0.03mol) zinc chloride to it, and heat up to 100°C Left and right, reflux reaction for 20 hours, HPLC tracking sample, after the reaction, start to drop the temperature, add 200ml water to it for washing, separate the lower water layer, wash the organic layer with 100ml saturated saline, separate the brine layer, and obtain the organic layer Be the toluene solution 160g of valsartan methyl ester crude product, contain valsartan methyl ester 22%.
- Preparation of valsartan methyl ester sodium salt
In a 3000ml four-neck flask, add 1000g of valsartan methyl ester toluene solution (cyclization reaction solution prepared in Example 1, containing 22% of valsartan methyl ester), then add the solution made of 60g sodium bicarbonate and 540g water , stirred at room temperature to form a salt for 4 hours, filtered, washed with 100g of toluene, and then washed with 100g of water, and dried in vacuum at 80°C to constant weight to obtain 220g of white valsartan methyl ester sodium salt.
- Preparation of Valsartan
Add 100g of valsartan methyl ester sodium salt into a 1000ml four-neck flask, then add 250g of 10% sodium hydroxide solution, keep warm at 25-30°C for 6 hours, adjust the pH value to 2-3 with 10% dilute hydrochloric acid, and then use acetic acid The product was extracted three times with ethyl ester, each time using 300ml. The organic layers were combined, washed once with 300ml of water, washed once with 300ml of saturated brine, dried with 30g of anhydrous magnesium sulfate, filtered, and evaporated to dryness at 60°C to obtain 92.5g of crude valsartan (detected by HPLC, chemical purity was 99.4%; manual HPLC detection, the optical purity was 97.8%).
Add 500ml of ethyl acetate to the crude product, heat to 50°C to dissolve, then cool to 0-5°C to crystallize for 2 hours, filter, wash, and dry to obtain 83g of valsartan (HPLC detection, chemical purity is 99.8%; chiral HPLC detection , the optical purity is 99.7%), and the total yield of hydrolysis crystallization is 90%.
- Valsartan – WikiPedia
- Li Hongfei. (2013). Observation on the curative effect of valsartan and amlodipine tablets in the treatment of 64 elderly hypertensive patients. Chongqing Medicine, 42(8), 926-927.
Valsartan Supplier and Manufacturer
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