Diastereoselective titanium enolate aldol reaction for the total synthesis of epothilones.
[formula: see text] The development of a highly diastereoselective addition of the titanium enolate derived from ketone 1 to aldehyde 2 offers an efficient entry to the total synthesis of the epothilone family. The new aldol process is robust and tolerates a wide range of functional groups.
Koch
Guido
G
Novartis Pharma AG, Process R&D and BU Oncology, Postfach CH-4002 Basel, Switzerland. guido.koch@pharma.novartis.com
Loiseleur
Olivier
O
Fuentes
Daniel
D
Jantsch
Andrea
A
Altmann
Karl-Heinz
KH
D000447:Aldehydes / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry; D034261:Epothilones / Q000138:chemical synthesis* / Q000737:chemistry; D013237:Stereoisomerism; D014025:Titanium / Q000737:chemistry
D000447:Aldehydes; D000970:Antineoplastic Agents; D034261:Epothilones; D014025:Titanium; C093788:epothilone B