Synthesis of benzothiazepines
Methods for preparing the following compound are disclosed.
1. A method for preparing the compound
comprising the step of preparing the compound
from 3-hydroxy-4-methoxythiophenol.
2. The method of claim 1 wherein said 3-hydroxy-4-methoxythiophenol is prepared from 2-methoxyphenyl acetate.
3. The method of claim 1 wherein said 3-hydroxy-4-methoxythiophenol is converted to
4. The method of claim 3 wherein the depicted structure is prepared as the corresponding dibenzoyl-L-tartrate salt.
5. The method of claim 3 wherein the depicted structure is prepared as the corresponding di-p-toluoyl-L-tartrate salt.
6. The method of claim 1 wherein said 3-hydroxy-4-methoxythiophenol is converted to
which is then converted to
via a Ritter reaction.
7. The method of claim 6 wherein said Ritter reaction uses ClCH 2 CN.
8. The method of claim 1 wherein said 3-hydroxy-4-methoxythiophenol is converted to
9. The method of claim 8 wherein said conversion includes reaction of said 3-hydroxy-4-methoxythiophenol with (R)-2-ammonio-2-ethylhexyl sulfate.
10. The method of claim 1 wherein said 3-hydroxy-4-methoxythiophenol is converted to
which is then converted to
which is then converted to
which is then converted to