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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 31, 2001 - Issue 16
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Original Articles

A GENERAL PROCEDURE FOR THE SYNTHESIS OF ACYLGUANIDINES DERIVED FROM ALIPHATIC AND AROMATIC AMINES

Seetharamaiyer Padmanabhan Cambridge NeuroScience Inc., One Kendall Square, Bldg. 700, Cambridge, MA, 02139, U.S.A.
,
Ruth C. Lavin Cambridge NeuroScience Inc., One Kendall Square, Bldg. 700, Cambridge, MA, 02139, U.S.A.
,
Paresh M. Thakkar Genetics Institute, 85 Bolton Street, Cambridge, MA, 02140, U.S.A.
&
Graham J. Durant Cambridge NeuroScience Inc., One Kendall Square, Bldg. 700, Cambridge, MA, 02139, U.S.A.
Pages 2491-2497 | Received 10 Nov 2000, Published online: 09 Nov 2006
 
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Abstract

Condensation of aliphatic and aromatic amines with 1-aroyl- S-methylisothiourea in the presence of triethylamine affords acylguanidines in moderate to good yields. An improved procedure for the generation of 1-aroyl-S-methylisothiourea derivatives is described.

ACKNOWLEDGMENT

The authors wish to thank M. E. Perlman, Lu Zhang, Aine Cullinan and Deke Moore for the HPLC purity determination of the products.

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