Asymmetric synthesis of the enkephalinase inhibitor thiorphan
摘要：
Independent enantioselective synthesis of (R)- and (S)-thiophan (1) via a six-step sequence has been completed. The pivotal step in the establishment of absolute stereochemistry in the enantiomeric target structures was the alkylation of the oxazolidyl carboximide-derived enolates 6 and 7 with bromomethyl benzyl sulfide (5b). The diastereoselection observed in these bond constructions was in excess of 95%.
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DOI：
10.1021/jo00211a008
被引量：
年份：
1985
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