Exo- and diastereo-selective synthesis of himbacine analogs
View Patent ↗This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
1. A compound of any of the following formulae:
wherein R 1 is selected from the group consisting of OR 2 and NR 3 R 4 , and R 2 , R 3 and R 4 are each independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, alkylaryl, and arylalkyl.
2. A compound of any of the following formulae:
wherein R 5 and R 6 are each independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, alkylaryl, and arylalkyl.
3. A compound selected from the group consisting of:
4. A compound which is