Selective and clean synthesis of aminoalkyl-H-phosphinic acids from hypophosphorous acid by phospha-Mannich reaction

Abstract

Acetic acid was used as a new solvent for phospha-Mannich reaction leading to clear reaction mixtures and high yields of the aminoalkylphosphonous acids (AHPA), and hydroxymethylated species were suggested as key intermediates in the reaction.

Polymorphism of amantadinium niflumate

“…11 Amantadine is a substance used in the treatment of Parkinson's disease and Parkinson's syndromes, as well as a drug against influenza A virus. 16,17 In the CSD there are some crystal structures of amantadine salts with bioactive components such as: indomethacin in conjunction with L-amino acids, 18 sulfamethoxazole, 19 [1-(dibenzylamino)ethyl] phosphonic acid, 20 fumaric acid, 21 oxalic acid, 4-aminobenzoic acid, glutaric acid, saccharin, 22 gemfibrozil, 23 sulfathiazole, 24 resveratrol, 25 and 3,7,12trihydroxycholan-24-oic acid 26 as well as salts with NSAIDs: indomethacin, diclofenac, and mefenamic, meclofenamic, flufenamic, tolfenamic acids. 27 In this paper we present two polymorphic structures of a new salt of niflumic acid with amantadine, which may be a potential new form of medicine exhibiting a synergistic therapeutic effect due to a change in properties.…”