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Bictegravir

Bictegravir structure

CAS No:
1611493-60-7
Formula:
C21H18F3N3O5
Chemical Name:
Bictegravir
Synonyms:
Bictegravir;GS-9883;(2R,5S,13aR)-2,3,4,5,7,9,13,13a-Octahydro-8-hydroxy-7,9-dioxo-N-[(2,4,6-trifluorophenyl)methyl]-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide;Bictegravir (GS-9883);(2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide;BNKY010-BC03;BICTEGRAVIR;GS-9883;GS 9883;GS9883;(2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Bictegravir (BIC) is a second-generation integrase strand transfer inhibitor (InSTI), like dolutegravir, with higher genetic barrier to resistance than raltegravir and elvitegravir.Bictegravir is a human immunodeficiency virus (HIV) integrase strand transfer inhibitor, the fourth in this class of agents that target the viral integrase. Bictegravir is used only in combination with other antiretroviral agents in the treatment of HIV infection and it has had limited use. Bictegravir is associated with a low rate of serum aminotransferase elevations during therapy, but has not been linked to instances of acute, clinically apparent liver injury.

ChEBI: Bictegravir is a monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxylic acid with the amino group of 2,4,6-trifluorobenzylamine. It is a second-generation integrase strand transfer inhibitor (INSTI) and used (as its sodium salt) for the treatment of HIV-1. It has a role as a HIV-1 integrase inhibitor. It is a monocarboxylic acid amide, a secondary carboxamide, a trifluorobenzene and an organic heterotetracyclic compound. It is a conjugate acid of a bictegravir(1-).

Bictegravir Basic Attributes

Molecular Weight：

449.38

Exact Mass：

449.38

Color/Form：

White to Off-White

Characteristics

PSA：

100.87

XLogP3：

1.9632

Density：

1.62±0.1 g/cm3(Predicted)

Melting Point：

>130°C (dec.)

Boiling Point：

682.5±55.0 °C(Predicted)

PKA：

4.50±1.00(Predicted)

Critical Temperature & Pressure：

Sealed in dry,Store in freezer, under -20°C

Bictegravir Use and Manufacturing

Bictegravir, is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.

Synthesis Route

1616340-75-0

1611493-60-7

Suppliers(18)

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