ChemInform Abstract: 3‐Benzo(b)furyl‐ and 3‐Benzo(b)thienylaminobutyric Acids as GABAB Ligands. Synthesis and Structure‐Activity Relationship Studies.

Abstract

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Synthesis of γ‐Aminobutyric Acid Analogs

“…Reductive dechlorination and subsequent enantioselective deprotonation with the lithium (S,S 0 )-di(a-methylbenzyl)amide (S,S 0 )- (107) and trapping of the resulting enolate with triethylsilyl chloride provided the silylenol ether (R)- (108). A one-pot ozonolysis and reductive amination afforded (R)-(3) [94].…”

“…[96]. The synthesis of a wide range of baclofen analogs has also been described including the phosphonic analog, phaclofen [97], iodobaclofen [98], heterocyclic analogs [99,100], hydroxysaclofen [101,102], homologs [103][104][105][106], pyrolidinone analogs [107], and conformationally restricted derivatives [108,109]. A highly efficient three-step synthesis of the phosphonic analog of baclofen, (AE)-phaclofen (114a) [110] and its a,a-difluoro analog (114b) has been reported (Scheme 14.32) [111].…”