Process for the synthesis of substituted carbodiimides

Details Process for the synthesis of substituted carbodiimides Process for the synthesis of substituted carbodiimides

1996-01-16

1997-07-15

Clardy, S. Mark

Organic compounds -- part of the class 532-570 series

Organic compounds

Amino nitrogen containing

C07C26700

Patent

active

056485379

ABSTRACT:
The invention relates to a new process for the synthesis of a disubstituted carbodiimide, including a first stage of phosgenation of an N,N'-disubstituted urea in an organic solvent medium.
After this first stage ammonia is added to the reaction mixture without preliminary isolation of any intermediate compound.
The process is simple, relatively inexpensive and the yield is high.
Disubstituted carbodiimides are organic synthesis intermediates used especially in pharmaceutical chemistry as coupling agents in peptide synthesis.

REFERENCES:
patent: 3301895 (1967-01-01), Sayigh et al.
patent: 4263221 (1981-04-01), Schnabel et al.
Tetrahedon, vol. 37, 1981, Oxford GB, pg. 233-284, M. Mikolajczyk "Recent developments in carbodiimide chemistry".
Chemische Berichte, vol. 91, 1958, Weinheim De, pp. 1992-1995, J. Macholdt-Erdniss "Eine enifache Darstellung aromatischer Guanidine".
Angewandte Chemie, vol. 72, No. 22, 1960, Eilingsfeld et al.
Journal of Organic Chemistry, vol.29, 1964, Easton US, pp. 2401-2404, H. Ulrich et al. "Syntheses and some reactions of allophanoyl chlocrides".

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