Patent ID: 8598346

Claim:
Method for preparation of cyclic amidines of formula I with R1, R2, R3, R4, R5, R6, R 7 =H, optionally substituted alkyl, cycloalkyl, aryl, heteroaryl, alkylaryl, arylalkyl, alkoxyalkyl, alkylthioalkyl, aryloxyalkyl or arylthioalkyl comprised of the following steps: bromination of a lactone of formula II to a dibromine compound of formula III esterification of the dibromine compound III to a compound IV amination of the dibromine compound IV to a diamino compound V and reaction of the compound V with an ortho-ester of formula R1-C(OR 18 ) 3 , with R1 having the meaning and importance outlined hereinabove and R 18 =alkyl, or an imidate of formula with R1, R 18 having the meaning and importance as outlined hereinabove, or a thioimidate of formula with R1, R 18 having the meaning and importance as outlined hereinabove, to obtain a cyclic amidine of formula I.