A trans or cis ethenyl group has been inserted between the α-carbon and the carboxyl group of α-aminoacids by Horner stereoselective olefination of α-aminoaldehydes. Numerous pure cis and trans vinylogous α-aminoacids have been obtained thus and coupled with aminopartners by classical methods. The versatility of the method was illustrated by the preparation of a [trans vinylogous-Gly3]Leu-enkephalin
Enantioselective synthesis of α,β-unsaturated γ- and δ-lactams
作者:Claude Grison、Stéphane Genève、Philippe Coutrot
DOI:10.1016/s0040-4039(01)00561-5
日期:2001.6
An enantioselective synthesis of alpha,beta -unsaturated gamma- and delta -lactams was proposed based on a simple strategy using the initial preparation of c is vinylogous aminoesters by the Horner reaction followed by a mild intramolecular cyclisation. (C) 2001 Elsevier Science Ltd. All rights reserved.
Novel enzymatic process for the manufacture of Boc-Dap-Oh priority to related application(s)
申请人:Iding Hans
公开号:US20080003652A1
公开(公告)日:2008-01-03
The present invention relates to a process for making a compound of formula (I)
The process involves the use of an enzyme. Compounds of formula (I) are intermediates in the manufacture of Dolastatin 10 analogues, which are useful in the treatment of cancer.
US6737409B2
申请人:——
公开号:US6737409B2
公开(公告)日:2004-05-18
Dolastatin 10 derivatives
申请人:——
公开号:US20030055002A1
公开(公告)日:2003-03-20
Novel anti-tumor compounds of formula,
1
are disclosed. Also disclosed are pharmaceutical compositions comprising compounds of formula (I), the use of compounds of formula (I) for the treatment of cancer, and processes for the preparation of compounds (I).