Synthesis 2015; 47(05): 653-658
DOI: 10.1055/s-0034-1379709
paper
© Georg Thieme Verlag Stuttgart · New York

Stereoselective Total Synthesis of Pinolide and Its C2 Epimer and Evaluation of Their Cytotoxic Activity[1]

Paramesh Jangili
a   Natural Products Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India   Email: biswanathdas@yahoo.com
,
C. Ganesh Kumar
b   Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India
,
Y. Poornachandra
b   Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India
,
Biswanath Das*
a   Natural Products Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India   Email: biswanathdas@yahoo.com
› Author Affiliations
Further Information

Publication History

Received: 19 September 2014

Accepted after revision: 19 November 2014

Publication Date:
11 December 2014 (online)


Abstract

Pinolide, a naturally occurring nonenolide and its C2 epimer have been synthesized using d-mannitol and 1,2-epoxyhex-5-ene as the starting materials. The synthesis involves the Jacobsen’s hydrolytic kinetic resolution, Yamaguchi esterification, and intramolecular ring-closing metathesis as the key steps. The 2-epi-pinolide, the C2 epimer of pinolide, has been synthesized for the first time. The cytotoxic activity of the pinolide and 2-epi-pinolide has been studied.