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Updated: Jun 4, 2026

A Direct, Early Stage Guanidinylation Protocol for the Synthesis of Complex Aminoguanidine-containing Natural Products
Published on: September 9, 2016
2-aminomethylphenylamine as a novel scaffold for factor Xa inhibitor
Akiyoshi Mochizuki1, Tsutomu Nagata, Hideyuki Kanno
1Research and Development Division, Daiichi Sankyo Co., Ltd, Edogawa-ku, Tokyo, Japan. mochizuki.akiyoshi.yk@daiichisankyo.co.jp
Abstract:
We have been researching orally active factor Xa inhibitor for a long time. We explored the new diamine linker using effective ligands to obtain a new attractive original scaffold 2-aminomethylphenylamine derivative. Compound 1D showed very strong in vitro and in vivo factor Xa inhibitory activity, as well as favorable PK profiles in po administration to monkeys.
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