Title:
The method for composition of activated ethyl fumarate, and its use as an intermediate
Document Type and Number:
Japanese Patent JP6241682
Kind Code:
B2
Abstract:
Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphophoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.
Inventors:
Craft, kelly
Freeman, John
Selvinsky, Paul
Pavia, Vinnie
Otto
Car, nabneet
Freeman, John
Selvinsky, Paul
Pavia, Vinnie
Otto
Car, nabneet
Application Number:
JP2015508969A
Publication Date:
December 06, 2017
Filing Date:
March 15, 2013
Export Citation:
Assignee:
Mankind Corporation
International Classes:
C07D241/08
Foreign References:
| CN101851213A | ||||
| US5503852 |
Other References:
N Kaur et al,A Delineation of diketopiperazine self-assembly process: understanding the molecular events involved in N-(fumaroyl)diketopiperazine of L-Lys(FDKP) interactions,Molecular Pharmaceutics,2008年,5(2),294-315
Attorney, Agent or Firm:
Kawaguchi International Patent Office