C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 265/18 (2006.01) C07C 211/52 (2006.01) C07C 213/00 (2006.01) C07C 213/02 (2006.01) C07C 215/68 (2006.01) C07C 217/58 (2006.01)
Patent
CA 2285000
The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1- benzoxazin-2-one of formula (VI-i) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In an embodiment, the present invention provides a process for the preparation of an amino alcohol compound of formula (V-i) comprising adding a toluene solution of 2,3-dichloro-5,6-dicyano-1,4-benzoquinone to a toluene solution of a compound of formula (III-i), via a compound of formula (IV-i).
Nouveaux procédés pour la synthèse asymétrique de (S)-6-chloro-4-cyclopropyléthynyl-4-trifluorométhyl-1,4-dihydro-2H-3,1-benzoxazin-2-one de formule (VI-i), qui est utile comme inhibiteur de la transcriptase inverse du virus de l'immunodéficience humaine (VIH). Dans un mode de réalisation, l'invention concerne un procédé pour préparer un composé amino-alcool de formule (V-i), consistant à ajouter une solution de toluène de 2,3-dichloro-5,6-dicyano-1,4 benzoquinone à une solution de toluène d'un composé de formule (III-i) via un composé de formule (IV-i).
Chen Cheng Y.
Choudhury Anusuya
Pierce Michael E.
Radesca Lilian A.
Tan Lushi
Chen Cheng Y.
Choudhury Anusuya
Dimock Stratton Llp
Dupont Pharmaceuticals Company
Merck & Co. Inc.
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