New 2-aminomethyl-4-cyanothiazole, prepared from thioamide and bromopyruvate ester, used as intermediate for serine protease inhibitors, e.g. thrombin inhibitors

摘要

2-Aminomethyl-4-cyanothiazole (I) and its salts are new. 2-Aminomethyl-4-cyanothiazoleof formula (I) and its salts are new. n = 0 or 1; and X = Cl, Br, SO3CF3, HSO4 or 1/2 SO4. Independent claims are included for: (1) the preparation of (I); (2) methods for preparing thiazolecarboxylate ester or amide intermediates of formula (VI) or (VII); and (3) new N-protected derivatives of (I) having formula (X). R3 = benzyloxycarbonyl, 9-fluorenylmethoxycarbonyl, trifluoromethylacetyl, acetyl or benzoyl. R1 = 1-4C alkyl.