COMPOSITION AND METHOD FOR NEUROPEPTIDE S RECEPTOR (NPSR) ANTAGONISTS
申请人:RESEARCH TRIANGLE INSTITUTE
公开号:US20150057268A1
公开(公告)日:2015-02-26
Neuropeptide S receptor antagonists are provided that bind in functional assays to neuropeptide S receptors; methods are provided for use of these antagonists in treatment of conditions or disease states that are ameliorated by blocking of the neuropeptide S receptor, including substance abuse and substance abuse relapse; and for use of neuropeptide S receptor antagonists in the manufacture of therapeutics and pro-drugs for therapeutics useful in disease states and conditions sensitive to binding of the neuropeptide S receptor.
A series of unsaturated alpha-amino alcohols were prepared via the allylboration of the corresponding N-protected alpha-amino ketones. The reactions are stereoselective, producing the syn isomers. The diastereoselectivity is not dramatically effected by the electronic nature of the N-protecting group or the reaction temperature but is dependent on the steric requirements of the N-protecting group and the solvent system.