Abstract:
:Racemic N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide (BM-5), a putative postsynaptic agonist and presynaptic antagonist at muscarinic receptors, was resolved into the enantiomers by a new method suitable for large scale preparation. The method involves a chemoselective N-debenzylation as the key step. The enantiomers of BM-5 were obtained after six separate steps in 25% overall yield. The ability of the enantiomers to release acetylcholine was evaluated in vivo by use of brain dialysis. (R)-BM-5 was the more potent enantiomer in this assay.
journal_name
Chiralityjournal_title
Chiralityauthors
Nilsson BM,De Boer P,Grol CJ,Hacksell Udoi
10.1002/chir.530040607subject
Has Abstractpub_date
1992-01-01 00:00:00pages
367-76issue
6eissn
0899-0042issn
1520-636Xjournal_volume
4pub_type
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