Copper-Catalyzed Aliphatic C–H Amination with an Amidine Moiety
摘要:
A method for amination of aliphatic C-H bonds of N-alkylamidines is described that utilizes Cu(OAc)(2) as the catalyst in the presence of Phl(OAc)(2) and K3PO4. The resulting products, dihydroimidazoles and tetrahydropyrimidines, could be converted into the corresponding diamines by hydride reduction.
Copper-Catalyzed Aliphatic C–H Amination with an Amidine Moiety
摘要:
A method for amination of aliphatic C-H bonds of N-alkylamidines is described that utilizes Cu(OAc)(2) as the catalyst in the presence of Phl(OAc)(2) and K3PO4. The resulting products, dihydroimidazoles and tetrahydropyrimidines, could be converted into the corresponding diamines by hydride reduction.
AMPHOTERICIN B DERIVATIVES WITH IMPROVED THERAPEUTIC INDEX
申请人:The Board of Trustees of the
University of Illinois
公开号:EP3055030A1
公开(公告)日:2016-08-17
[EN] AMPHOTERICIN B DERIVATIVES WITH IMPROVED THERAPEUTIC INDEX<br/>[FR] DÉRIVÉS D'AMPHOTÉRICINE B AYANT UN INDICE THÉRAPEUTIQUE AMÉLIORÉ
申请人:UNIV ILLINOIS
公开号:WO2015054148A1
公开(公告)日:2015-04-16
Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea derivatives of AmB. Certain of the derivatives are C3, C5, C8, C9, C11, C13, or C15 deoxy derivatives of AmB. Certain of the derivatives include C3' or C4' modifications of the mycosamine appendage of AmB. Also provided are methods of making AmB derivatives of the invention, pharmaceutical compositions comprising AmB derivatives of the invention, and methods of use of AmB derivatives of the invention.