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(11)    Patent No :    AP 1985    (73) Applicant(s)       
(21)    Application No :    AP/P/2006/003603    TIBOTEC PHARMACEUTICALS LTD., Little Island , Co Cork,       
            Ireland       
                   
(22)    Filing Date :    30.09.2004           
(24)    Date of Grant &    30.03.2009           
                   
(45)    Publication :

(30)  Priority Data    (72) Inventors

    (33) Country    (31) Number    (32) Date    DE KOCK Herman Augustinus, Belgium   
    EP            03103630.4    30.09.2003    FILLIERS Walter Ferdinand Maria, Belgium   
    US            60/507,996        02.10.2003       
                            AELTERMAN Wim Albert Alex, Belgium   
                                   
                                et al       
                                (74) Representative   
(84)    Designated State                   
                           
    BW    GM    GH    KE    LS    MW    MZ   NA   SL    HONEY & BLANCKENBERG   
    SD    SZ    T Z    UG    ZM    ZW               
(51)    International    Classification    C07D263/58 (2006.01)    C07D417/12 (2006.01)   
                            C07D413/12 (2006.01)       
(54    Title

Methods for the preparation of benzoxazole sulfonamide compounds and intermediates thereof

(57)    Abstract

The present invention relates to methods for the preparation of benzoxazole sulfonamide compounds of formula (9) as well as novel intermediates of formula (6) for use in said method. More in particular the invention relates to methods for the Preparation of 2-amino-benzoxazole sulfonamide compounds which make use of 2-mercapto-benzoxazole sulfonamide intermediates, more in particular methods employing the intermediate

1-Benzyl-2-hydroxy -3-[isobutyl(2-methylsulfanyl-benzoxazole -6-sul-fonyl)-ami no)-propyl)-carbamic ester, and to methods amenable to industrial scaling up. Said benzoxazole sulfonamide compounds are particularly useful as HIV protease inhibitors. The substituents are defined in the claims.


(56)    Documents Cited :    WO 02/092595 A    WO 01/77092 A

 

 

 

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