Heterocyclic core analogs of a direct thrombin inhibitor was written by Blizzard, Timothy A.;Singh, Sanjay;Patil, Basanagoud;Chidurala, Naresh;Komanduri, Venukrishnan;Debnath, Samarpita;Belyakov, Sergei;Crespo, Alejandro;Struck, Alice;Kurtz, Marc;Wiltsie, Judyann;Shen, Xun;Sonatore, Lisa;Arocho, Marta;Lewis, Dale;Ogletree, Martin;Biftu, Tesfaye. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2014.Reference of 86069-86-5 The following contents are mentioned in the article:
Thrombin is a serine protease that plays a key role in blood clotting. Pyrrolidine I•TFA is a potent thrombin inhibitor discovered at Merck several years ago. Seven analogs of I•TFA in which the pyrrolidine core was replaced with various heterocycles were prepared and evaluated for activity against thrombin, clotting factors VIIa, IXa, Xa, and XIIa, and trypsin. The thiomorpholine analog II•TFA was the most active, essentially matching the thrombin inhibitory activity of I•TFA with slightly improved selectivity over trypsin. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Reference of 86069-86-5).
(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Reference of 86069-86-5
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem