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Asymmetric Synthesis of Norcantharidin Analogues by Alkynylation of Oxabenzonorbornadienes and Their Anticancer Activities

Summary: The present invention relates to chemical entities originated from natural sources or obtained from a chemically synthesized compound and further synthesized for therapeutic uses. More particularly, the present invention relates to norcantharidin analogues synthesized by a transition metal-catalyzed alkynylation of oxanorbornadiene derivatives and their antitumor effects.

Technology Benefits: Reducing the side-effect in the urinary system to some extent and increasing the number of white blood cells with comparable anti-cancer activity

Technology Application: Used as an anticancer agent in clinical application

Detailed Technology Description: The norcantharidin analogues of the present invention are originated from natural sources and further synthesized into at least three different compounds. using an Ir catalyst to carry out transition metal-catalyzed alkynylation of oxanorbornadiene derivatives.

Supplementary Information: Inventor: Chan, Albert Sun-Chi | Fan, Baomin | Wang, Jun | Lin, Chengyuan | Huang, Chao | Yang, Qingjing | Xu, Jianbin | Bian, Zhaoxiang | Lu, Aiping | Hu, Jun
Priority Number: US8835658B2
IPC Current: C07D030700 | C07D049308
US Class: 549459
Assignee Applicant: Hong Kong Baptist University
Title: Asymmetric synthesis of norcantharidin analougus by alkynylation of oxabenzonorbornadienes and their anticancer activities
Usefulness: Asymmetric synthesis of norcantharidin analougus by alkynylation of oxabenzonorbornadienes and their anticancer activities
Summary: (I) is useful for treating cancer tumors including colorectal carcinoma and breast adenocarcinoma (all claimed). Test details are described but no results given.
Novelty: Synthesizing norcantharidin compounds, useful for treating cancer tumors e.g. colorectal carcinoma, comprises alkynylation of oxabenzonorbornadienes in presence of catalyst including transition metal compound and biaryl diphosphine ligand

Industry: Disease Diagnostic/Treatment

Sub Category: Cancer/Tumor

Application Date: 2012.12.28

Application No.: US 13/729,479

Others: Filed

ID No.: G06/CY/Lipp/US01

Country/Region: Hong Kong

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