TY - JOUR
T1 - Comparing the greenness and sustainability of three routes to an HIV protease inhibitor intermediate
AU - Akakios, Stephanie Gina
AU - Bode, Moira Leanne
AU - Sheldon, Roger Arthur
PY - 2021
Y1 - 2021
N2 - The greenness and sustainability of three different routes for the synthesis of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-ol (bis-furan alcohol), an advanced intermediate for a group of HIV protease inhibitors, including the FDA approved darunavir, used in antiretroviral (ARV) therapy, were compared. The method involved a comparison of (i) waste generated using theE-factor and relative to industrial benchmarks using the innovative Green Aspiration Level (iGAL™) method, (ii) solvent usage on the basis of solvent intensity (SI) and properties according to the GSK solvent guide, and (iii) Green Motion™ scores according to the MANE methodology.
AB - The greenness and sustainability of three different routes for the synthesis of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-ol (bis-furan alcohol), an advanced intermediate for a group of HIV protease inhibitors, including the FDA approved darunavir, used in antiretroviral (ARV) therapy, were compared. The method involved a comparison of (i) waste generated using theE-factor and relative to industrial benchmarks using the innovative Green Aspiration Level (iGAL™) method, (ii) solvent usage on the basis of solvent intensity (SI) and properties according to the GSK solvent guide, and (iii) Green Motion™ scores according to the MANE methodology.
UR - http://www.scopus.com/inward/record.url?scp=85105849989&partnerID=8YFLogxK
U2 - 10.1039/d1gc00986a
DO - 10.1039/d1gc00986a
M3 - Article
AN - SCOPUS:85105849989
SN - 1463-9262
VL - 23
SP - 3334
EP - 3347
JO - Green Chemistry
JF - Green Chemistry
IS - 9
ER -