Studies on Anti-Helicobacter pylori Agents. Part 1: Benzyloxyisoquinoline Derivatives

Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-Isoquinolinylguanidines

“…The 1-chloro intermediates were either known compounds (4-CH 3 , 12 5-OCH 3 , 12 7-OCH 3 , 12 4-Cl, 13 4-Br, 14 5-Br 15 ) or were prepared from the corresponding isoquinoline by oxidation with either 30% H 2 O 2 /AcOH or mCPBA/CH 2 Cl 2 , followed by treatment of the N-oxide with POCl 3 (5-C 6 H 5 , 16 5-OCH 2 C 6 H 5 , 17 6-Br, 18 7-OCH 2 C 6 H 5 19 ). In the case of 5-bromo-1-chloro-and 7-bromo-1-chloroisoquinolines, a mixture of 5-and 7-bromoisoquinoline 20 was oxidized, the product was treated with POCl 3 and the mixture of chloro compounds was separated by fractional crystallization from THF at )78°C to give the individual isomers 3e and 3j (Scheme 2).…”

Synthetic approaches to 2-aryl/hetaryl- and 2-(hetaryl)ylidene derivatives of fluorinated 1,3-benzothiazin-4-ones

“…2,6-Difluorobenzoic acid 1, 2,3,4,5-tetrafluorobenzoyl chloride 10a and pentafluorobenzoyl chloride 10b were purchased from Merck (CAS numbers 385-00-2, 94695-48-4, 2251-50-5). 3-Nitro-2,6-difluorobenzoic acid 2 was synthesized according to the literature [9]. Procedure for toluene solution of 2,6-difluoro-3-nitrobenzoylchloride 3 was reported [8].…”

Synthesis and kinase inhibitory potencies of new pyrido[3,4-g]quinazolines substituted at the 8-position

“…TLC Rf = 0.7 (EtOAc/Cyclohexane 1:4). 1 (8). To a solution of 7 (1.0 g, 2.63 mmol) and but-3-yn-1-ol (0.50 mL, 6.50 mmol) in Et3N (10 mL), under argon atmosphere, were added PdCl2(PPh3)2 (36 mg, 0.052 mmol) and CuI (20 mg, 0.105 mmol).…”