Sonja Mackey - Galesburg MI, US Michael Matison - Kalamazoo MI, US Haifeng Wu - Portage MI, US Paul Herrinton - Portage MI, US Michael Goble - San Diego CA, US Moses McMillian - Portage MI, US Vikram Kalthod - Mattawan MI, US
International Classification:
C07C311/35
US Classification:
564/086000
Abstract:
A process for preparing (S)-(-)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide (IIa) with fluoroamine (III) in the presence of triacetoxyborohydride and ethyl acetate to provide [4-[4-[ethyl(6-fluoro-6-metylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide (I) anll then converting I into the hemifumarate salt Ia. A process for preparing IIa is also claimed as well as intermediates IIa-lId.
Compounds And Methods For Preparing Methanesulfonamides
Sonja MacKey - Galesburg MI, US Michael Matison - Kalamazoo MI, US Haifeng Wu - Portage MI, US Michael Goble - San Diego CA, US Moses McMillan - Portage MI, US Vikram Kalthod - Mattawan MI, US
International Classification:
C07C311/13
US Classification:
564097000
Abstract:
A process for preparing (S)-(−)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxylphenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4-[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide(IIa) with fluoroamine (III) in the presence of triacetoxyborohydride and ethyl acetate to provide [4-[-4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxylphenyl]methanesulfonamide(I) and then converting I into the hemifumarate salt Ia. A process for preparing IIa is also claimed as well as intermediates IIa-IId.
- Wesborough MA, US Bertrand L. CHENARD - Waterford CT, US Yuelian XU - East Haven CT, US Roberta L. DOROW - Kalamazoo MI, US Michael E. MATISON - Middleville MI, US Alexander KOLCHINSKI - Winchester MA, US Richard FORNICOLA - Littleton MA, US
The present invention provides compounds that inhibit Factor XIa or kallikrein and pharmaceutically acceptable salts thereof and compositions thereof. The present invention also provides methods of making these compounds or pharmaceutically acceptable salts thereof and compositions and methods of use thereof.
- Westborough MA, US Bertrand L. Chenard - Waterford CT, US Yuelian Xu - East Haven CT, US Roberta L. Dorow - Kalamazoo MI, US Michael E. Matison - Middleville MI, US Alexander Kolchinski - Winchester MA, US Richard Fornicola - Littleton MA, US
International Classification:
C07D 401/06 A61P 7/02 A61L 33/04 A61L 33/00
Abstract:
Provided herein are compounds and compositions that inhibit Factor XIa or kallikrein and methods of using these compounds and compositions.