Process for preparing intermediates for thrombin inhibitors

Details Process for preparing intermediates for thrombin inhibitors Process for preparing intermediates for thrombin inhibitors

1995-05-18

1997-03-11

Ivy, C. Warren

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

540454, 540470, 540480, 540481, 540544, 540596, 540597, 540575, 540602, 544 60, 544129, 544141, 544365, 544372, 546189, 548518, C07D21160

Patent

active

056103085

ABSTRACT:
A process is provided for preparing intermediates of the structure ##STR1## wherein Rpg is preferably .dbd.CHC.sub.6 H.sub.5 ; and P.G. is a protecting group CBZ or BOC, wherein a protected guanylpyrazole is reacted with an azacycloalkyl, azacycloalkenyl or azaheteroalkyl derivative (such as a piperidine derivative) in the presence of a DBU catalyst. The resulting intermediate may be used as a starting material for preparing thrombin inhibitors.

REFERENCES:
patent: 5498724 (1996-03-01), Nystrom et al.
Bernatowicz, M. S. et al, "Urethane Protected Derivatives of 1-Guanylpyrazole for the Mild and Efficient Preparation of Guanidines", Tetrahedron Letters, vol. 34, No. 21, pp. 3389-3392 (1993).

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