Herbert Richard Anderson

US Patent:

61601314, Dec 12, 2000

Filed:

Dec 17, 1998

Appl. No.:

9/213192

Inventors:

Yuh-Meei Lin - Naperville IL
Herbert M. Anderson - Woodridge IL
Tuah R. Jenta - Chicago IL
Michael J. Williams - Ottawa IL
Michael T. Flavin - Darien IL
Ze-Qi Xu - Naperville IL

Assignee:

Sarawak Medichem Pharmaceuticals, Inc. - Lemont IL

International Classification:

C07D31178
C07D40714

US Classification:

549277

Abstract:

An efficient and scalable method is reported for the isolation of costatolide (2), an HIV-1-specific nonnucleoside reverse transcriptase inhibitor (NNRTI), from the latex of Calophyllum plants such as C. teysmannii var. inophylloide. An overall yield of 10. 6% of costatolide, with a purity of 96%, was obtained by repetitive recrystallization of the latex from a single organic solvent after the oily material was removed by treatment with hexane. A second major component of the latex, soulattrolide (3), another HIV-1 NNRTI, was also isolated. Both compounds were characterized by spectroscopic and chromatographic analyses and their in vitro anti-HIV activities were also confirmed. The results suggest that sufficient supplies of costatolide can be obtained in a relatively low-cost manner from natural sources.