148766-15-8Relevant articles and documents
Antineoplastic agents. 599. Total synthesis of dolastatin 16
Pettit, George R.,Smith, Thomas H.,Arce, Pablo M.,Flahive, Erik J.,Anderson, Collin R.,Chapuis, Jean-Charles,Xu, Jun-Ping,Groy, Thomas L.,Belcher, Paul E.,Macdonald, Christian B.
, p. 476 - 485 (2015)
The first 23-step total synthesis of the cyclodepsipeptide dolastatin 16 (1) has been achieved. Synthesis of the dolaphenvaline and dolamethylleuine amino acid units using simplified methods improved the overall efficiency. The formation of the 25-membere
Intermediate for preparing halichondrin compound and preparation method thereof
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Paragraph 0132-0135, (2020/07/07)
The invention relates to an intermediate for preparing a halichondrin compound and a preparation method thereof. The invention particularly relates to an intermediate for preparing halichondrin, eribulin or analogues thereof, and a preparation method and application of the intermediate. The intermediate as well as the preparation method and application thereof are used for constructing C20-C26 structural fragments of the halichondrin compound. The initial raw materials of the synthesis route are cheap, easy to obtain, stable in source and reliable in quality; the structural characteristics ofreactants are fully utilized in the selection of a chiral center construction method, so that the synthesis efficiency is practically improved, and the difficulty and risk of product quality control are reduced; and the use of a high-toxicity and expensive organic tin catalyst is avoided, so that the cost and the environmental friendliness are remarkably improved.
Nucleophilic halo-michael addition under lewis-base activation
Laina-Martín, Víctor,Pérez, Ignacio,Fernández-Salas, Jose A.,Alemán, José
supporting information, p. 12936 - 12939 (2019/11/05)
A simple and general conjugate nucleophilic halogenation is presented. The THTO/halosilane combination has shown the ability to act as a nucleophilic halide source in the conjugate addition to a variety of Michael acceptors. In addition, a straightforward diastereoselective halogen installation using α,β-unsaturated acyloxazolidinones as platforms has been developed.