706819-80-9Relevant articles and documents
5-Iodo-3-ethoxypyrazoles: An entry point to new chemical entities
Guillou, Sandrine,Janin, Yves L.
scheme or table, p. 4669 - 4677 (2010/08/06)
Our program, which has focused on the preparation of new pyrazole derivatives, has led us to report here an original and simplified preparation of ethyl 3-ethoxy-lW-pyrazole-4-carboxylate. This is based on the reaction of hydrazine monohydrochloride and diethyl 2-(ethoxymethylene)malonate. Further transformations of this key compound allowed the preparation of the two possible iodinated isomers, namely, 3-ethoxy-4-iodo- and 3-ethoxy-5-iodo-1H-pyrazole. These compounds have opened the way to a quick access to many original pyrazole series. As an illustration, we report here on the selectivity of N-arylation, by using the Lam and Cham method, the C4- and C5-arylation of some of these 3-ethoxy-pyrazole derivatives by using the Suzuki-Miyaura reaction, and C5-benzylation reactions by means of the Negishi reaction. This was followed by hydrolysis of the ethoxy group, which led to the corresponding pyrazol-3-one derivatives. As a conclusion of this work, we conducted an investigation into the regiochemistry of the condensation between diethyl 2-(ethoxymethylene) malonate and the hydrochloride salts of methyl, benzyl, or phenyl hydrazine.
A novel series of potent and selective small molecule inhibitors of the complement component C1s
Subasinghe, Nalin L.,Ali, Farah,Illig, Carl R.,Rudolph, M. Jonathan,Klein, Scott,Khalil, Ehab,Soll, Richard M.,Bone, Roger F.,Spurlino, John C.,DesJarlais, Renee L.,Crysler, Carl S.,Cummings, Maxwell D.,Morris Jr., Philip E.,Kilpatrick, John M.,Babu, Y. Sudhakara
, p. 3043 - 3047 (2007/10/03)
Activation of the classical pathway of complement has been implicated in disease states such as hereditary angioedema, ischemia-reperfusion injury and acute transplant rejection. The trypsin-like serine protease C1s represents a pivotal upstream point of
