Phosphorylation of terminal primary alcohol groups

Details Phosphorylation of terminal primary alcohol groups Phosphorylation of terminal primary alcohol groups

C - Chemistry, Metallurgy

07

F

C07F 9/09 (2006.01) C07D 413/12 (2006.01) C07D 413/14 (2006.01) C07F 9/6558 (2006.01) C07F 9/6574 (2006.01)

Patent

CA 2395052

The invention relates to chemical processes and chemical intermediates which are useful in the selective formation of a primary mono-phosphoryl group (- OPO(OH2)) in a terminal 1,2-diol-propanoyl (HO-CH2CH(OH)-CO-) containing system, and to chemical processes and chemical intermediates (and processes for their manufacture) particularly useful for the manufacture of anti-Gram positive oxazolidinone bacterial agents containing such functionality, in particular for the preparation of 5(R)-Isoxazol-3-yloxymethyl-3-(4-(1-(2(S) - hychoxy-3-phosphoryl-propanoyl)-1,2,5,6-tetrahydropyridy-4-il)3,5- difluorophenyl)oxazolidin-2-one.

L'invention porte sur des processus chimiques et des intermédiaires chimiques s'avérant efficaces pour la formation sélective d'un groupe mono-phosphoryle primaire (-OPO(OH¿2?)) dans un système à terminaison 1,2-diol-propanoyl (HO-CH¿2?CH(OH)-CO-), et sur des processus chimiques et des intermédiaires chimiques (et leurs procédés d'obtention) s'avérant particulièrement efficaces pour la préparation d'agents d'oxazolidinone anti bactéries Gram positifs présentant une telle fonctionnalité, et en particulier pour la préparation de 5(R)-isoxazol-3-yloxyméthyl-3-(4-(1-(2(S)-hydroxy-3-phosphoryl-propanoyl)-1,2,5,6-tétrahydropyridy-4-yl)-3,5-difluorophényl)oxazolidin-2-one.

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