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Practical synthesis of (S)-pyrrolidin-2-yl-1H-tetrazole, incorporating efficient protecting group removal by flow-reactor hydrogenolysis

Research output: Contribution to journalJournal article

Published

Journal publication date4/04/2006
JournalSynlett
Journal number6
Volume2006
Number of pages4
Pages889-892
Original languageEnglish

Abstract

A practical, safe, high-yielding and efficient synthesis of (S)-pyrrolidin-2-yl-1H-tetrazole has been developed, which avoids the generation of ammonium azide in the cyclisation step and the use of a 9:1 acetic acid-water mixture as the solvent in the hydrogenation. The previously extended hydrogenolysis reaction time (three days) is now reduced to hours through the use of an H-Cube (TM) (a continuous-flow reactor employing a mixed hydrogen-liquid flow stream).