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Synthetic Studies toward the Natural Product Tripartin, the First Natural Histone Lysine Demethylase Inhibitor.

ABSTRACT: An efficient synthesis of dimethyl tripartin as a synthetic precursor of natural product tripartin, the first natural specific inhibitor of histone H3 lysine 9 demethylase KDM4, is described. The synthesis of dimethyl tripartin was achieved in a six-step longest linear sequence starting from commercially available 3,5-dimethoxy benzaldehyde with 21% overall yield, using ClTi(O ⁱ Pr)₃-mediated dichloromethine insertion as the key step.

SUBMITTER: Dethe DH

PROVIDER: S-EPMC6645238 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature

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Synthetic Studies toward the Natural Product Tripartin, the First Natural Histone Lysine Demethylase Inhibitor.

Dethe Dattatraya H DH Boda Raghavender R

ACS omega 20180816 8

An efficient synthesis of dimethyl tripartin as a synthetic precursor of natural product tripartin, the first natural specific inhibitor of histone H3 lysine 9 demethylase KDM4, is described. The synthesis of dimethyl tripartin was achieved in a six-step longest linear sequence starting from commercially available 3,5-dimethoxy benzaldehyde with 21% overall yield, using ClTi(O i Pr)3-mediated dichloromethine insertion as the key step. ...[more]

PMID: 31459063

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