Hangzhou JINLAN Pharm-Drugs Technology Co., Ltd

1. Core Identifiers Generic Name: Eteiravir English Abbreviation: EVG CAS Number: 697761-98-1 Chemical Name: (4R,12aS)-9-[(2,4-difluorophenyl)methyl]-4,6-dimethyl-8-[(1-methyl-1H-1,2,4-triazol-5-yl)carbonyl]-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazin-7(5H)-one Molecular Formula: C₂₄H₂₆F₂N₆O₃ Molecular Weight: 484.50 g/mol Chemical Structural Characteristics: Belongs to the INSTI class of oxazinopyrazinones. The molecule contains 3 key active structures that determine its ability to target integrase: β- Ketoamide group (8-position triazole carboxyl group): forms a coordination bond with the two Mg²⁺ ions in the active site of HIV-1 integrase, which is the core of inhibiting chain transfer activity; 2,4-difluorobenzyl side chain (9-position): inserts into the hydrophobic pocket of the integrase, and forms hydrophobic interactions with amino acids such as Trp132 and Tyr143, enhancing binding affinity; Chiral oxazine ring (4R, 12aS configuration): only this chiral configuration can correctly match the conformation of the active site of the integrase. Other chiral isomers (such as 4S, 12aR) have no inhibitory activity, and chiral purity must be strictly controlled.