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.
Enantiospecific synthesis of 3-pyrrolines: A route to novel polyhydroxylated pyrrolidines
作者:Ian Burley、Alan T. Hewson
DOI:10.1016/0040-4039(94)88236-3
日期:1994.9
Enantiopure acetamido ketones are converted by an intramolecular Wittig reaction into enantiopure 3-pyrrolines; the product from (S)-serine provides access to novelpolyhydroxylatedpyrrolidines.
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.