C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 7/56 (2006.01) A61K 38/12 (2006.01) C07F 9/40 (2006.01) C07H 13/00 (2006.01) C07K 1/113 (2006.01)
Patent
CA 2301184
The present invention provides phosphonylating agents and phosphonylation conditions that are compatible with the acid- and base-sensitive compounds and which promote a regioselective and reproducible conversion to a phosphonate compound. Also provided are intermediates that may be used to prepare phosphonate derivatives of cyclic peptides antifungal agent and a process for converting the phosphonates to the desired phosphonic acid prodrugs.
La présente invention concerne des agents et des conditions de phosphonylation compatibles avec les composés sensibles aux acides et aux bases et favorisant une conversion reproductible et régiosélective en un composé de phosphonate. L'invention concerne également des intermédiaires pouvant être utilisés pour préparer des dérivés de phosphonate d'un agent antifongique à base de peptides cycliques, et un procédé permettant de convertir les phosphonates en les promédicaments désirés à base d'acide phosphonique.
Grutsch John Leo Junior
Hansen Marvin Martin
Harkness Allen Robert
Udodong Uko Effiong
Verral Daniel Edward II
Eli Lilly And Company
Gowling Lafleur Henderson Llp
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