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An improved multigram synthesis of tetradeuterated buspirone
Author(s) -
Vashishtha S. C.,
McKay G.,
Midha K. K.
Publication year - 1999
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(199910)42:10<919::aid-jlcr245>3.0.co;2-w
Subject(s) - chemistry , buspirone , alkylation , piperazine , yield (engineering) , hydrochloride , combinatorial chemistry , bioavailability , organic chemistry , stereochemistry , pharmacology , biochemistry , catalysis , medicine , materials science , receptor , metallurgy , agonist
A simple, convenient and efficient two step method for the synthesis of buspirone‐d 4 hydrochloride 4 from the commercially available materials is described. Tetramethylene glutarimide 1 was first N‐alkylated with 1,4‐dibromobutane‐2,2,3,3‐d 4 2 to give a monoalkylated compound 3 which was transformed to buspirone‐d 4 by alkylation with 1‐(2‐pyrimidyl)piperazine. This important antianxiety compound obtained in 63% yield having isotopic purity ∽96% should prove useful in carrying out bioavailability studies. Copyright © 1999 John Wiley & Sons, Ltd.