(R)-3-ethynyl-3-hydroxy-1-methylpyrrolidin-2-one → HCID 86693421, compound

Participants

Reaction Steps

Ethyl 9-bromo-8-fluoro-4-hydroxy-4,5-dihydrobenzo[2,3]oxepino[4,5-d]thiazole-2-carboxylate was reacted with (3R)-3-ethynyl-3-hydroxy-1-methyl-pyrrolidin-2-one similarly to as described in General Procedure F to afford ethyl 8-fluoro-4-hydroxy-9-(((R)-3-hydroxy-1-methyl-2-oxopyrrolidin-3-yl)ethynyl)-4,5-dihydrobenzo[2,3]oxepino[4,5-d]thiazole-2-carboxylate which was directed subjected to General Procedure M to afford 12.9 mg and 17.1 mg (22% overall yield) after reverse phase purification then chiral separation. The absolute stereochemistry at the 4-hydroxyl substitution position for each isomer was not determined.

Provenance & Evidence