“…However, compared with asymmetric alkynylation of aldehydes, [4d, 5] efficient catalytic systems for alkynylation of ketones [6] to generate propargylic alcohols with tetrasubstituted stereogenic centers remain underdeveloped, largely because of the low reactivity of metalated terminal alkynes toward ketones. For enantioselective alkynylation of isatins, [7–9] efficient catalytic systems, such as CuI/chiral guanidine, CuI/chiral phosphine ligand, Zn(OTf) 2 /chiral hydroxyl oxazoline ligand, AgOAc/chiral phase‐transfer catalyst, CuOTf/bisoxazolidine, and Co(OAc) 2 /bisoxazolinephosphine have been developed by the groups of Liu, [7a] Guo, [7b] Chen, [7c] Maruoka, [7d] Wolf, [7e] and Li, [7f] respectively. 3‐Alkynyl‐3‐hydroxy‐2‐oxindoles generated by alkynylation of isatins have been found to exhibit important biological activities (Scheme 1 b).…”