Bictegravir CAS 1611493-60-7 Pharma Powder Raw Materials

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Bictegravir Powder  Usage and Synthesis.

Bictegravir Powder is an antiviral drug used primarily to treat hepatitis B and C virus infections. Bictegravir CAS 1611493-60-7 is a nucleoside analogue that is recognized by viral RNA polymerase and embedded in viral RNA, preventing viral replication and spread. It is often used with other drugs, such as ribavirin and sofosbuvir, to improve the effectiveness of treatment.Bictegravir Raw Materials (BIC) is a novel integrase inhibitor.

Bictegravir (BIC) is a second-generation integrase strand transfer inhibitor (INSTI) approved in combination with emtricitabine and tenofovir alafenamide at fixed doses for HIV treatment, with potent antiviral activity INSTIs in vitro against wild-type viruses and strains with first-generation resistance.

Pharmacological Action of Bictegravir Powder:

Bictegravir is cleared from the liver primarily by cytochrome P4503A4 (CYP3A4) oxidation and UDP-glucuronosyltransferase 1A1 (UGT1A1) glucuronidation. Therefore, potent inducers of UGT1A1 and CYP3A4 (e.g., rifamycin/anticonvulsants) should be avoided due to the significantly reduced serum exposure to biketilide chemicalbookvir. Chelation with multivalent cations reduces absorption; otherwise, drug-drug interactions are rare.

Preparation of Bictegravir Powder.

• Step 1: 1-(2,2-Dimethoxyethyl)-5-methoxy-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid (1-A, 3.15 g, 10.0 mmol) suspended in acetonitrile (36 mL) and acetic acid (4 mL) was treated with methanesulfonic acid (0.195 mL). The mixture was heated to 75 °C. After 7 h, the crude mixture was cooled and stored at -10 °C for three days. The crude mixture was heated again to 75 °C for 2 h, cooled, and used in the next step without purification.
• Step 2: Crude 1-(2,2-dihydroxyethyl)-5-methoxy-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid (16.8 mL of crude mixture from step 1, about 4 mmol) was mixed with (1S,3R)-3-aminocyclopentanol (0.809 g, 8 mmol), diluted with acetonitrile (16.8 mL) and treated with potassium carbonate (0.553 g, 4 mmol) was treated. The reaction mixture was heated to 85°C, stirred for 15 min, cooled to ambient temperature and stirred for another 16 h. HCl (50 mL, 0.2 Maq) was added and the clear yellow solution was extracted three times with dichloromethane. The combined organic layers were dried over sodium sulfate, filtered and concentrated to a yellow solid. The precipitate crude material from dichloromethane/hexane gives the desired intermediate 15-B as a light beige powder.

• Step 3: Compound 15-B (38 mg, 0.12 mmol) was dissolved in 1 mL of acetonitrile and treated with 2,4,6-trifluorophenylmethylamine (34 mg, 0.21 mmol), HATU (50 mg, 0.13 mmol), N,N-diisopropylethylamine (DIPEA) (23 mg, 0.18 mmol) and stirred at room temperature for 2 for 2 h, after which LCMS analysis showed complete consumption of compound 15-B and formation of intermediate 45-A. The reaction mixture was carried over to the next step.

• Step 4: To the crude reaction solution of the previous step, MgBr2 (55 mg, 0.30 mmol) was added. The reaction mixture was stirred at 50 °C for 1 h. The reaction mixture was acidified with 10% HCl aqueous solution, partitioned between aqueous solution and dichloromethane and the aqueous phase was extracted with dichloromethane. The combined organic phases were dried over MgSO4, filtered, concentrated and purified by HPLC (ACN/H2O containing 0.1% TFA modifier) to give Compound 45 over bictegravir.

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