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1. (WO2014191457) METHODS OF SYNTHESIS OF INGENOL AND INTERMEDIATES THEREOF

Pub. No.:    WO/2014/191457    International Application No.:    PCT/EP2014/061053
Publication Date: Fri Dec 05 00:59:59 CET 2014 International Filing Date: Thu May 29 01:59:59 CEST 2014
IPC: C07C 29/42
C07C 29/00
C07C 35/28
C07D 317/70
C07C 45/30
C07C 45/40
C07C 45/64
C07C 45/65
C07C 45/72
C07C 49/743
C07C 17/02
C07C 49/693
C07C 49/627
C07C 49/727
C07C 47/21
Applicants: LEO LABORATORIES LIMITED
Inventors: BARAN, Phillipe S.
JØRGENSEN, Lars
KUTTRUFF, Christian A.
MCKERRALL, Steven J.
YEH, Chien-Hung
Title: METHODS OF SYNTHESIS OF INGENOL AND INTERMEDIATES THEREOF
Abstract:
The present invention relates generally to methods of synthesis of diterpene heterocylic compounds. More particularly, the present invention relates to efficient methods of synthesis of ingenol (Formula (21), CAS 30220-46-3), from a compound of formula (1). The present invention also provides for various advantageous intermediates along the synthetic route of ingenol. Efficient synthesis of ingenol is important in the design and synthesis of related analogues, such as ingenol-3-angelate.