- Alkoxypyrazoles and the process for their preparation
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The present invention relates to a process for the preparation of alkoxypyrazoles and new alkoxypyrazole compounds.
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Page/Page column 13; 16
(2010/03/02)
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- 5-Iodo-3-ethoxypyrazoles: An entry point to new chemical entities
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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.
- Guillou, Sandrine,Janin, Yves L.
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experimental part
p. 4669 - 4677
(2010/08/06)
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- A novel series of potent and selective small molecule inhibitors of the complement component C1s
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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
- 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
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p. 3043 - 3047
(2007/10/03)
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