We disclose an efficient procedure for the preparation of ethers of 2-substituted 2-hydroxymethylpyrroline and of 2-aminomethyl-3-pyrrolines, involving, as a key step, formation and nucleophilic ring opening of a cyclic sulfamidate. Several new analogs of epibatidine (1) and tebanicline (ABT-594, 2) were prepared and tested for analgesic activity in the mouse formalin model.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.bmcl.2005.01.058 | DOI Listing |
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!