An efficient total synthesis of (+)-Pancratistatin via a highly stereoselective intramolecular Henry reaction

An efficient total synthesis of (+)-Pancratistatin via a highly stereoselective intramolecular Henry reaction

(+)-Pancratistatin, first isolated in 1984 from the bulbs of Hawaiian Hymenocallis littoralis, displays remarkable antineoplastic and anticancer properties. Recently Xu, Liu and Coll. published an efficient gram-scale total synthesis of (+)-Pancratistatin based on a highly stereoselective intermolecular Michael addition and intramolecular Henry reaction to build the cyclohexane ring C containing six successive chiral centers. [1] The intramolecular Henry reaction is presented in the Scheme below.

DFT calculations were performed to analyze this intramolecular Henry reaction.

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[1] F. Ding, L. Liang, J. Yao, B. Wang, C. Xu, D. Liu, Org. Lett. 2022, 24, 9458-9462.

Aisha Khalifa

PhD organic and medicinal & polymer chemistry

2 个月

Interesting

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Dr.Vishnuvardhan Nomula

Organic chemistry &Peptide, carbohydrates synthesis

2 个月

Nice chemistry

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Rakeshwar Bandichhor Ph.D. FRSC, CChem, SSWB,BB,MB

Vice President & Head, Chemistry - API - Process R&D at Dr. Reddy's Laboratories, Vice-Chair, ACS-India Chapter (South India), Organic Process Research & Development (OPRD), ACS-Editorial Advisory Board Member

2 个月

Nice Chemistry! Loved it

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NavNath Kalamkar

Life Sciences & Drug development

2 个月

One of the highly promising nature’s gifted compound for cancer therapies. Pharma & Biotech companies need more attention on this or analogues molecules.

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