The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Mar. 03, 1998

Filed:

Nov. 10, 1994
Applicant:
Inventors:

Oleg Werbitzky, Visp, CH;

Ulrich Daum, Hofstetten, CH;

Rachel Bregy, Raron, CH;

Assignee:

Lonza Ltd., Gampel/Valais, CH;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D / ; C07D / ; C07D / ;
U.S. Cl.
CPC ...
540567 ; 544282 ; 544245 ; 5483027 ; 5483017 ; 540555 ;
Abstract

The process for the preparation of bicyclic amidines of the general formula: ##STR1## wherein A is selected from the group consisting of --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --, --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 -- and --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 --CR.sup.9 R.sup.10 --, wherein the substituents in A are in each case numbered starting from the nitrogen atom, and B is selected from the group consisting of --CR.sup.11 R.sup.12 --CR.sup.13 R.sup.14 --, --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.13 R.sup.14 -- and --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.17 R.sup.18 --CR.sup.13 R.sup.14 --, and R.sup.1, R.sup.2 and R.sup.11 to R.sup.14 are, in each case independently of one another, hydrogen, C.sub.1 -C.sub.4 -alkyl, aryl, or are C.sub.1 -C.sub.4 -alkyl which is substituted with hydroxyl, amino, C.sub.1 -C.sub.4 -alkylamino or mercapto, and R.sup.3 to R.sup.10 and R.sup.15 to R.sup.18 are, in each case independently of one another, hydrogen, C.sub.1 -C.sub.4 -alkyl, aryl, hydroxyl, amino, C.sub.1 -C.sub.4 -alkylamino or mercapto, or are C.sub.1 -C.sub.4 -alkyl which is substituted with hydroxyl, amino, C.sub.1 -C.sub.4 -alkylamino or mercapto. The process includes heating (reacting) a lactone of the general formula: ##STR2## wherein A is as defined above, to at least 150.degree. C. together with an at least equimolar quantity of an amine of the general formula:


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