C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 243/04 (2006.01) C07D 317/28 (2006.01) C07D 323/00 (2006.01) C07D 401/00 (2006.01) C07D 403/00 (2006.01) C07D 405/00 (2006.01) C07D 409/00 (2006.01) C07D 413/00 (2006.01) C07D 417/00 (2006.01) C07D 453/02 (2006.01) C07D 455/02 (2006.01) C07D 471/04 (2006.01) C07D 473/00 (2006.01) C07D 475/00 (2006.01) C07D 491/04 (2006.01) C07D 495/04 (2006.01) C07D 498/04 (2006.01) C07D 513/04 (2006.01) C07F 5/02 (2006.01) C07F 9/645 (2006.01) C07F 9/6558 (2006.01) C07K 1/113 (2006.01)
Patent
CA 2222132
Disubstituted cyclic ureas IV are prepared by reductive alkylation of I with aldehydes R22-CHO or R23-CHO in presence of a reducing agent to form II (step 1), followed by cyclocarbonylation of II to form III (step2) and deprotection of III to form the diol IV (step 3), according to the above schemes. These cyclic ureas IV are useful as HIV protease inhibitors.
L'invention porte sur des urées (IV) cycliques disubstituées préparées par alkylation réductrice de (I) par des aldéhydes R?22¿-CHO ou R?23¿-CHO en présence d'un agent réducteur qui donne (II) (première étape), suivie d'une cyclocarbonylation de (II) qui donne (III) (deuxième étape) et d'une déprotection de (III) qui donne le diol (IV) (troisième étape), conformément au schéma. Lesdits urées (IV) cycliques s'avèrent d'utiles inhibiteurs des protéases du VIH.
Confalone Pasquale Nicholas
Smyser Thomas Edgar
Bristol-Myers Squibb Pharma Company
Dimock Stratton Llp
The Dupont Merck Pharmaceutical Company
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