1-Azoniabicyclo[3.3.0]oct-1(5)-ene salt derivatives and process for the preparation of the same
申请人:SANWA KAGAKU KENKYUSHO CO., LTD.
公开号:EP0484702A1
公开(公告)日:1992-05-13
There are described 1-azoniabicyclo[3.3.0]oct-1(5)-ene salt derivatives of formula (I) inclusive of 1-azonia-4,6-dimethylbicyclo[3.3.0]oct-1 (5)-ene perchlorate, and a process for the preparation of the same. The derivatives can be prepared by heating dicyclopropylmethanimine salt derivative in a solvent, in the presence or absence of an ammonium salt. Each of the derivatives is employed as an intermediate for preparing various medicines and agricultural chemicals.
Syntheses and Reactions of Some Cyclopropyl-substituted Imines. Part 2. Structural and Conformational Properties of Dicyclopropylketimine as Studied by Microwave Spectroscopy and Quantum Chemical Calculations.
作者:Louis A. Carpino、Khaled Nasr、Adel Ali Abdel-Maksoud、Ayman El-Faham、Dumitru Ionescu、Peter Henklein、Holger Wenschuh、Michael Beyermann、Eberhard Krause、Michael Bienert
DOI:10.1021/ol901310q
日期:2009.8.20
The N-dicyclopropylmethyl (Dcpm) residue, introduced into amino acids via reaction of dicyclopropylmethanimine hydrochloride with an amino acid ester followed by sodium cyanoborohydride or triacetoxyborohydride reduction, can be used as an amide bond protectant for peptide synthesis. Examples which demonstrate the amelioration of aggregation effects include syntheses of the alanine decapeptide and the prion peptide (106-126). Avoidance of cyclization to the aminosuccinimide followed substitution of Fmoc-(Dcpm)Gly-OH for Fmoc-Gly-OH in the assembly of sequences containing the sensitive Asp-Gly unit.
1-azoniabicyclo[3.3.0]oct-1(5)-ene salt derivatives and process for the
申请人:Sanwa Kagaku Kenkyusho Co., Ltd.
公开号:US05110945A1
公开(公告)日:1992-05-05
There are described 1-azoniabicyclo[3.3.0]oct-1(5)-ene salt derivatives inclusive of 1-azonia-4,6-dimethylbicyclo[3.3.0]oct-1(5)-ene perchlorate, and a process for the preparation of the same. The derivatives can be prepared by heating dicyclopropylmethanimine salt derivative in a solvent, in the presence or absence of an ammonium salt. Each of the derivatives is employed as an intermediate for preparing various medicines and agricultural chemicals.