@article {47047,
	title = {Ru-catalyzed asymmetric transfer hydrogenation of alpha-acyl butyrolactone via dynamic kinetic resolution: asymmetric synthesis of bis-THF alcohol intermediate of darunavir},
	journal = {Tetrahedron Letters},
	volume = {66},
	year = {2021},
	month = {MAR },
	pages = {152831},
	type = {Article},
	abstract = {<p>The Ru-catalyzed enantio- and diastereoselective dynamic kinetic resolution of alpha-(benzyloxy/benzoyloxy)acyl-gamma-butyrolactones has been examined via transfer hydrogenation. Employing the in situ prepared (R,R)-Ru-FsDPEN catalyst, the transfer hydrogenation of using formic acid/triethylamine at rt gave the corresponding (S)-3-((S)-2-(benzyloxy/benzoyloxy)-1-hydroxyethyl)dihydrofuran-2(3H)-on e with good to excellent diastereo- and enantioselectivity. One of the resulting hydrogenation product prepared on gram scales was utilized for the synthesis of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol (1), a key synthetic intermediate of various HIV protease inhibitors such as darunavir with excellent enantio-(95\% ee) and diastereoselectivities (dr 95:5). (C) 2021 Elsevier Ltd. All rights reserved.</p>
},
	keywords = {Bis-THF-OH intermediate, Darunavir, Dynamic kinetic resolution, Ru-catalysis, transfer hydrogenation},
	issn = {0040-4039},
	doi = {10.1016/j.tetlet.2021.152831},
	author = {More, V. Ganesh and Malekar, V. Pushpa and Kalshetti, Rupali G. and Shinde, Mahesh H. and Ramana, V. Chepuri}
}
@article {48677,
	title = {Rh-catalyzed C-H functionalization of the (Pyrazol-5-yl)pyridine core of GBT-440},
	journal = {Synthesis-Stuttgart},
	volume = {55},
	year = {2023},
	month = {NOV },
	pages = {3600-3609},
	type = {Article},
	abstract = {<p>
	The Rh-catalyzed cross dehydrogenative coupling (CDC)/alkylation of the pyrazolylpyridine unit of GBT-440 proceeded smoothly under ambient conditions and selectively on the pyrazole unit while directed by the pyridine. The scope of these reactions was established by employing simple as well as conjugated olefins for CDC and various diazo esters and the TIPS-EBX reagent for alkylation. At the outset, a focused small molecule library around the bis-heterocyclic core of GBT440 was developed via C-H functionalization.</p>
},
	keywords = {C-H activation, cross dehydrogenative coupling, diazo ester, GBT-440, Rh catalysis, TIPS-EBX},
	issn = {0039-7881},
	doi = {10.1055/a-2116-6734},
	author = {Kalshetti, Rupali G. and Halnor, Swapnil V. and Ramana, Chepuri V.}
}
