Diastereoselective Synthesis of 3-Fluoro-2-substituted Piperidines and Pyrrolidines
نویسندگان
چکیده
منابع مشابه
Enantioselective synthesis of 2-substituted and 3-substituted piperidines through a bromoaminocyclization process.
A catalytic enantioselective bromocyclization of olefinic amides using amino-thiocarbamates as the catalysts has been developed. The resulting enantioenriched 2-substituted 3-bromopiperidines can readily be transformed to 3-substituted piperidines through a silver salt-mediated rearrangement. This process has been applied to the synthesis of a dopaminergic drug, Preclamol.
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Substituted seven-membered N-heterocycles are prevalent bioactive epitopes and useful synthons for preparing enzyme inhibitors or molecular recognition systems. To fully exploit the chemical properties of this flexible N-heterocycle scaffold, efficient methods for its diverse functionalization are required. Here we utilize the late-stage oxidation of tetrahydroazepines as an approach to access ...
متن کاملDiastereoselective synthesis of substituted diaziridines from simple ketones and aldehydes.
Diastereopure substituted diaziridines from simple ketones, aldehydes and amines are here reported. These important chemical scaffolds are obtained in the presence of a weak inorganic base and hydroxylamine O-sulfonic acid (HOSA). This method introduces three stereocenters in one step to provide a wide variety of substituted diaziridines with high yields and diastereoselectivities.
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ژورنال
عنوان ژورنال: HETEROCYCLES
سال: 2014
ISSN: 0385-5414
DOI: 10.3987/com-13-s(s)27